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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 2,885 | 25-hydroxycholesterol | Metabolite | 6,597 | Agonist | Agonist | false | 135,651,392 | null | null | - | 11,425 | Journal | Mol Endocrinol | Structural basis for hydroxycholesterols as natural ligands of orphan nuclear receptor RORgamma. | 20,203,100 | null | PMC2870936 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 2,740 | ALRT 1550 | Synthetic organic | 6,401 | Antagonist | Antagonist | false | 135,649,927 | null | null | - | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 11,711 | AZD0284 | Synthetic organic | 88,265 | Agonist | Inverse agonist | false | 442,878,737 | false | 7.39 | pIC50 | 42,923 | Journal | Journal of Medicinal Chemistry | AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2 | 34,464,130 | 10.1021/acs.jmedchem.1c01197 | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,045 | cintirorgon | Synthetic organic | 85,456 | Agonist | Agonist | false | 375,973,233 | false | 6.3 | pEC50 | 35,963 | Patent | null | Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease | null | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,045 | cintirorgon | Synthetic organic | 85,457 | Agonist | Agonist | false | 375,973,233 | false | 6.3 | pEC50 | 35,963 | Patent | null | Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease | null | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 12,351 | compound 14 [Schnute <i>et al</i>., 2023] | Synthetic organic | 89,108 | Agonist | Inverse agonist | false | 479,821,142 | false | 8.03 | pIC50 | 44,589 | Journal | ACS Medicinal Chemistry Letters | Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists | null | 10.1021/acsmedchemlett.2c00500 | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,643 | compound 25 [Zhang <i>et a</i>l., 2020] | Synthetic organic | 87,032 | Allosteric modulator | Negative | false | 404,859,090 | false | 9 | pIC50 | 38,667 | Journal | ACS Med Chem Lett | Discovery of <i>N</i>-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases. | 32,071,676 | 10.1021/acsmedchemlett.9b00431 | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,528 | compound 32 [PMID: 31638797] | Synthetic organic | 86,838 | Agonist | Inverse agonist | false | 387,065,610 | false | 7.62 | pEC50 | 38,448 | Journal | J Med Chem | Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy. | 31,638,797 | null |
||
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,528 | compound 32 [PMID: 31638797] | Synthetic organic | 86,837 | Agonist | Inverse agonist | false | 387,065,610 | false | 10.44 | pIC50 | 38,449 | Patent | null | Tricyclic sulfones as rorϒ modulators | null | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 9,660 | GNE-3500 | Synthetic organic | 84,554 | Agonist | Inverse agonist | false | 348,353,619 | true | 7.92 | pEC50 | 33,537 | Journal | J Med Chem | Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist. | 26,061,388 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 9,661 | GSK2981278 | Synthetic organic | 84,555 | Agonist | Inverse agonist | false | 348,353,620 | true | 8.49 | pIC50 | 33,538 | Journal | PLoS ONE | Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin. | 26,870,941 | null | PMC4752338 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,642 | MRL-871 | Synthetic organic | 87,031 | Agonist | Inverse agonist | false | 404,859,089 | false | 7.8 | pEC50 | 38,666 | Journal | Bioorg Med Chem Lett | Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists. | 26,048,793 | null |
||
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,078 | RORC2 inverse agonist 66 [PMID: 30130103] | Synthetic organic | 85,526 | Agonist | Inverse agonist | false | 375,973,265 | false | 8.39 | pIC50 | 36,117 | Journal | J Med Chem | Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. | 30,130,103 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,078 | RORC2 inverse agonist 66 [PMID: 30130103] | Synthetic organic | 85,525 | Agonist | Inverse agonist | false | 375,973,265 | false | 7.78 | pIC50 | 36,118 | Patent | null | Methyl-and trifluoromethyl-substituted pyrrolopyridine modulators of rorc2 and methods of use thereof | null | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,143 | SR1001 | Synthetic organic | 85,728 | Agonist | Inverse agonist | false | 381,118,853 | true | 6.95 | pKi | 29,073 | Journal | Nature | Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. | 21,499,262 | null | PMC3148894 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,145 | SR1555 | Synthetic organic | 85,729 | Agonist | Inverse agonist | false | 381,118,855 | true | 6 | pIC50 | 36,408 | Journal | ACS Chem Biol | Identification of a selective RORγ ligand that suppresses T(H)17 cells and stimulates T regulatory cells. | 22,769,242 | PMC3448878 |
||
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,144 | SR2211 | Synthetic organic | 85,730 | Agonist | Inverse agonist | false | 381,118,854 | true | 6.98 | pKi | 36,409 | Journal | ACS Chem Biol | Identification of SR2211: a potent synthetic RORγ-selective modulator. | 22,292,739 | PMC3331898 |
||
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 2,755 | T0901317 | Synthetic organic | 87,029 | Agonist | Inverse agonist | false | 135,651,223 | false | 7.29 | pKi | 29,072 | Journal | Mol Pharmacol | The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist. | 19,887,649 | null | PMC2812071 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 9,867 | TAK-828F | Synthetic organic | 84,981 | Agonist | Inverse agonist | false | 363,894,161 | true | 8.72 | pIC50 | 34,599 | Journal | J Med Chem | Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist. | 29,510,038 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,366 | XY101 | Synthetic organic | 86,350 | Agonist | Inverse agonist | false | 384,403,646 | true | 7.52 | pIC50 | 37,666 | Journal | J Med Chem | Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. | 30,964,293 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,366 | XY101 | Synthetic organic | 86,351 | Agonist | Inverse agonist | false | 384,403,646 | true | 6.12 | pKd | 37,666 | Journal | J Med Chem | Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. | 30,964,293 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 600 | RAR-related orphan receptor-γ | 10,366 | XY101 | Synthetic organic | 86,352 | Agonist | Inverse agonist | false | 384,403,646 | true | 6.42 | pKd | 37,666 | Journal | J Med Chem | Discovery and Characterization of XY101, a Potent, Selective, and Orally Bioavailable RORγ Inverse Agonist for Treatment of Castration-Resistant Prostate Cancer. | 30,964,293 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 2,742 | 22R-hydroxycholesterol | Metabolite | 6,413 | Agonist | Agonist | false | 135,651,388 | null | 5.5 | pEC50 | 10,504 | Journal | J Pharmacol Exp Ther | Oxysterol 22(R)-hydroxycholesterol induces the expression of the bile salt export pump through nuclear receptor farsenoid X receptor but not liver X receptor. | 16,371,446 | null | PMC4114575 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 11,728 | BMS-986318 | Synthetic organic | 88,287 | Agonist | Agonist | false | 458,923,763 | false | 7.28 | pEC50 | 42,970 | Journal | ACS Med Chem Lett | Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis. | 34,531,950 | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 12,109 | BMS-986339 | Synthetic organic | 88,830 | Agonist | Agonist | false | 472,319,231 | false | 7.47 | pEC50 | 43,971 | Journal | J Med Chem | Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis. | 35,704,802 | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 608 | chenodeoxycholic acid | Metabolite | 6,410 | Agonist | Agonist | true | FDA (1983), EMA (2017) | 135,651,455 | true | 5.3 | pEC50 | 10,501 | Journal | Science | Bile acids: natural ligands for an orphan nuclear receptor. | 10,334,993 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 608 | chenodeoxycholic acid | Metabolite | 6,410 | Agonist | Agonist | true | FDA (1983), EMA (2017) | 135,651,455 | true | 5.3 | pEC50 | 10,502 | Journal | Mol Cell | Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. | 10,360,171 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 609 | cholic acid | Metabolite | 6,409 | Agonist | Agonist | true | EMA (2013), FDA (2015) | 135,651,459 | null | null | pEC50 | 10,502 | Journal | Mol Cell | Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. | 10,360,171 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 609 | cholic acid | Metabolite | 6,409 | Agonist | Agonist | true | EMA (2013), FDA (2015) | 135,651,459 | null | null | pEC50 | 10,501 | Journal | Science | Bile acids: natural ligands for an orphan nuclear receptor. | 10,334,993 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 10,644 | cilofexor | Synthetic organic | 87,033 | Agonist | Agonist | false | 404,859,091 | false | 7.6 | pEC50 | 38,682 | Patent | null | FXR (NR1H4) binding and activity modulating compounds | null | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 11,130 | compound 25 [PMID: 32687365] | Synthetic organic | 87,353 | Agonist | Agonist | false | 434,122,190 | false | 6.03 | pEC50 | 39,936 | Journal | J Med Chem | Design and Structural Optimization of Dual FXR/PPARδ Activators. | 32,687,365 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 10,187 | compound 3f [Festa <i>et al.</i>, 2019] | Synthetic organic | 85,848 | Antagonist | Antagonist | false | 381,118,897 | false | 6.24 | pIC50 | 36,680 | Journal | ACS Med Chem Lett | Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists. | 30,996,787 | 10.1021/acsmedchemlett.8b00534 | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 610 | deoxycholic acid | Metabolite | 6,411 | Agonist | Agonist | true | FDA (2015) | 135,651,468 | null | 4 | pEC50 | 5,353 | Journal | Neurosci Lett | U50,488, a kappa opioid receptor agonist, attenuates cocaine-induced increases in extracellular dopamine in the nucleus accumbens of rats. | 7,898,771 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 610 | deoxycholic acid | Metabolite | 6,411 | Agonist | Agonist | true | FDA (2015) | 135,651,468 | null | 4 | pEC50 | 10,501 | Journal | Science | Bile acids: natural ligands for an orphan nuclear receptor. | 10,334,993 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 610 | deoxycholic acid | Metabolite | 6,411 | Agonist | Agonist | true | FDA (2015) | 135,651,468 | null | 4 | pEC50 | 10,502 | Journal | Mol Cell | Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. | 10,360,171 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 2,744 | fexaramine | Synthetic organic | 6,415 | Agonist | Agonist | false | 135,650,259 | false | 6.6 | pEC50 | 10,506 | Journal | Mol Cell | A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. | 12,718,892 | null | PMC6179153 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 2,745 | guggulsterone | Natural product | 14,312 | Antagonist | Antagonist | false | 135,652,690 | false | null | pIC50 | 18,563 | Journal | Mol Endocrinol | The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptor. | 12,089,353 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 2,745 | guggulsterone | Natural product | 6,416 | Antagonist | Antagonist | false | 135,652,690 | false | 5 | pEC50 | 10,507 | Journal | Science | A natural product that lowers cholesterol as an antagonist ligand for FXR. | 11,988,537 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 2,743 | GW4064 | Synthetic organic | 6,414 | Agonist | Agonist | false | 135,650,334 | false | 7.8 | pEC50 | 10,505 | Journal | J Med Chem | Identification of a chemical tool for the orphan nuclear receptor FXR. | 10,956,205 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 12,910 | HPG1860 | Synthetic organic | 90,016 | Agonist | Agonist | false | 485,206,031 | false | 8.3 | pEC50 | 46,036 | Journal | J Med Chem | Discovery of HPG1860, a Structurally Novel Nonbile Acid FXR Agonist Currently in Clinical Development for the Treatment of Nonalcoholic Steatohepatitis. | 37,424,079 | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 10,198 | INT-767 | Synthetic organic | 85,864 | Agonist | Agonist | false | 381,118,908 | false | 7.52 | pEC50 | 36,732 | Journal | Mol Pharmacol | Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist. | 20,631,053 | PMC2981390 |
||
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 611 | lithocholic acid | Metabolite | 6,412 | Agonist | Agonist | false | 135,651,505 | null | 5.3 | pEC50 | 10,501 | Journal | Science | Bile acids: natural ligands for an orphan nuclear receptor. | 10,334,993 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 611 | lithocholic acid | Metabolite | 6,412 | Agonist | Agonist | false | 135,651,505 | null | 5.3 | pEC50 | 10,503 | Journal | Science | Identification of a nuclear receptor for bile acids. | 10,334,992 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 611 | lithocholic acid | Metabolite | 6,412 | Agonist | Agonist | false | 135,651,505 | null | 5.3 | pEC50 | 10,502 | Journal | Mol Cell | Endogenous bile acids are ligands for the nuclear receptor FXR/BAR. | 10,360,171 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 10,655 | nidufexor | Synthetic organic | 87,050 | Agonist | Partial agonist | false | 404,859,102 | false | 9.3 | pEC50 | 38,730 | Journal | J Med Chem | Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. | 31,940,200 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 3,435 | obeticholic acid | Synthetic organic | 7,983 | Agonist | Agonist | true | EMA & FDA (2016) | 178,100,437 | true | 7 | pEC50 | 14,212 | Journal | J Med Chem | 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. | 12,166,927 | null | null |
89 | nhr | 1H. Liver X receptor-like receptors | 603 | Farnesoid X receptor | 9,725 | tropifexor | Synthetic organic | 84,710 | Agonist | Agonist | false | 354,702,202 | false | 9.7 | pEC50 | 33,897 | Journal | J Med Chem | Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH). | 29,148,806 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 604 | Farnesoid X receptor-β | 2,802 | cholesten | Metabolite | 6,420 | Agonist | Agonist | false | 135,651,456 | null | 5 | pEC50 | 10,541 | Journal | Mol Cell Biol | Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol. | 12,529,392 | null | PMC140718 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 604 | Farnesoid X receptor-β | 2,748 | desmosterol | Metabolite | 6,419 | Agonist | Agonist | false | 135,651,470 | null | 5 | pEC50 | 10,541 | Journal | Mol Cell Biol | Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol. | 12,529,392 | null | PMC140718 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 604 | Farnesoid X receptor-β | 2,746 | lanosterol | Metabolite | 6,417 | Agonist | Agonist | false | 135,651,499 | null | 6 | pEC50 | 10,541 | Journal | Mol Cell Biol | Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol. | 12,529,392 | null | PMC140718 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 604 | Farnesoid X receptor-β | 2,747 | vitamin D3 | Metabolite | 6,418 | Agonist | Agonist | true | 135,651,594 | null | 5 | pEC50 | 10,541 | Journal | Mol Cell Biol | Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol. | 12,529,392 | null | PMC140718 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,742 | 22R-hydroxycholesterol | Metabolite | 6,421 | Agonist | Agonist | false | 135,651,388 | null | 5.3 | pEC50 | 10,554 | Journal | Nature | An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha. | 8,878,485 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,751 | 24(S), 25-epoxycholesterol | Metabolite | 6,423 | Agonist | Agonist | false | 135,651,390 | false | null | pEC50 | 10,553 | Journal | Proc Natl Acad Sci USA | Structural requirements of ligands for the oxysterol liver X receptors LXRalpha and LXRbeta. | 9,874,807 | null | PMC15128 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,751 | 24(S), 25-epoxycholesterol | Metabolite | 6,423 | Agonist | Agonist | false | 135,651,390 | false | null | pEC50 | 29,176 | Journal | Nat Chem Biol | Brain endogenous liver X receptor ligands selectively promote midbrain neurogenesis. | 23,292,650 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,751 | 24(S), 25-epoxycholesterol | Metabolite | 6,423 | Agonist | Agonist | false | 135,651,390 | false | null | pEC50 | 10,561 | Journal | J Biol Chem | Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. | 9,013,544 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,750 | 24(S)-hydroxycholesterol | Metabolite | 6,422 | Agonist | Agonist | false | 135,651,391 | null | 5.4 | pEC50 | 10,561 | Journal | J Biol Chem | Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. | 9,013,544 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,752 | 27-hydroxycholesterol | Metabolite | 6,424 | Agonist | Agonist | false | 135,651,393 | null | 7.1 | pEC50 | 10,549 | Journal | J Biol Chem | 27-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. | 11,504,730 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,753 | acetyl-podocarpic dimer | Synthetic organic | 6,427 | Agonist | Agonist | false | 135,649,888 | null | 9 | pEC50 | 10,574 | Journal | J Biol Chem | A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux. | 11,790,770 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 7,725 | AZ12260493 | Synthetic organic | 80,225 | Agonist | Agonist | false | 223,366,058 | true | 8.15 | pKi | 25,429 | Webpage | null | AZ12260493. | null | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,748 | desmosterol | Metabolite | 82,631 | Agonist | Agonist | false | 135,651,470 | false | 5.54 | pKi | 29,195 | Journal | J Biol Chem | Sterol intermediates from cholesterol biosynthetic pathway as liver X receptor ligands. | 16,857,673 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 8,690 | GSK2033 | Synthetic organic | 82,626 | Antagonist | Antagonist | false | 252,166,890 | false | 7 | pIC50 | 29,186 | Journal | J Med Chem | Discovery of tertiary sulfonamides as potent liver X receptor antagonists. | 20,345,102 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,754 | GW3965 | Synthetic organic | 6,428 | Agonist | Agonist | false | 135,650,333 | null | 6.7 | pEC50 | 10,546 | Journal | J Med Chem | Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. | 11,985,463 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 10,034 | IMB-808 | Synthetic organic | 85,439 | Agonist | Partial agonist | false | 375,973,222 | false | 6.82 | pEC50 | 35,889 | Journal | Mol Pharmacol | Identification of a Novel Liver X Receptor Agonist that Regulates the Expression of Key Cholesterol Homeostasis Genes with Distinct Pharmacological Characteristics. | 28,087,808 | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,688 | L-783483 | Synthetic organic | 6,426 | Agonist | Agonist | false | 135,650,496 | null | 7.9 | pKd | 10,566 | Journal | Endocrinology | A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a). | 12,072,387 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,309 | paxilline | Synthetic organic | 6,425 | Agonist | Agonist | false | 135,650,789 | null | 5.4 | pEC50 | 10,543 | Journal | J Pharmacol Exp Ther | A natural product ligand of the oxysterol receptor, liver X receptor. | 12,893,846 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 8,692 | SR9238 | Synthetic organic | 82,628 | Antagonist | Inverse agonist | false | 252,166,892 | false | 6.67 | pIC50 | 29,190 | Journal | ACS Chem Biol | A liver-selective LXR inverse agonist that suppresses hepatic steatosis. | 23,237,488 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 602 | Liver X receptor-α | 2,755 | T0901317 | Synthetic organic | 6,429 | Agonist | Agonist | false | 135,651,223 | null | 7.3 | pEC50 | 10,571 | Journal | Genes Dev | Role of LXRs in control of lipogenesis. | 11,090,131 | null | PMC317060 |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,742 | 22R-hydroxycholesterol | Metabolite | 6,430 | Agonist | Agonist | false | 135,651,388 | null | 5.52 | pEC50 | 10,554 | Journal | Nature | An oxysterol signalling pathway mediated by the nuclear receptor LXR alpha. | 8,878,485 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,751 | 24(S), 25-epoxycholesterol | Metabolite | 6,433 | Agonist | Agonist | false | 135,651,390 | false | null | pEC50 | 29,176 | Journal | Nat Chem Biol | Brain endogenous liver X receptor ligands selectively promote midbrain neurogenesis. | 23,292,650 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,751 | 24(S), 25-epoxycholesterol | Metabolite | 6,433 | Agonist | Agonist | false | 135,651,390 | false | null | pEC50 | 10,561 | Journal | J Biol Chem | Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. | 9,013,544 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,750 | 24(S)-hydroxycholesterol | Metabolite | 6,431 | Agonist | Agonist | false | 135,651,391 | null | 5.5 | pEC50 | 10,561 | Journal | J Biol Chem | Activation of the nuclear receptor LXR by oxysterols defines a new hormone response pathway. | 9,013,544 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,752 | 27-hydroxycholesterol | Metabolite | 6,432 | Agonist | Agonist | false | 135,651,393 | null | 7.15 | pEC50 | 10,549 | Journal | J Biol Chem | 27-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. | 11,504,730 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,753 | acetyl-podocarpic dimer | Synthetic organic | 6,437 | Agonist | Agonist | false | 135,649,888 | null | 9 | pEC50 | 10,574 | Journal | J Biol Chem | A potent synthetic LXR agonist is more effective than cholesterol loading at inducing ABCA1 mRNA and stimulating cholesterol efflux. | 11,790,770 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 7,725 | AZ12260493 | Synthetic organic | 80,226 | Agonist | Agonist | false | 223,366,058 | true | 7.96 | pKi | 25,422 | Webpage | null | AZD9291. | null | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 10,035 | compound 17l [PMID: 26288691] | Synthetic organic | 85,441 | Antagonist | Antagonist | false | 375,973,223 | false | 5.74 | pIC50 | 35,890 | Journal | ACS Med Chem Lett | Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators. | 26,288,691 | PMC4538439 |
||
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,748 | desmosterol | Metabolite | 82,632 | Agonist | Agonist | false | 135,651,470 | false | 5.85 | pKi | 29,195 | Journal | J Biol Chem | Sterol intermediates from cholesterol biosynthetic pathway as liver X receptor ligands. | 16,857,673 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 8,690 | GSK2033 | Synthetic organic | 82,625 | Antagonist | Antagonist | false | 252,166,890 | false | 7.5 | pIC50 | 29,186 | Journal | J Med Chem | Discovery of tertiary sulfonamides as potent liver X receptor antagonists. | 20,345,102 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 8,693 | GSK9772 | Synthetic organic | 82,629 | Allosteric modulator | Negative | false | 252,166,893 | false | 7.52 | pIC50 | 29,192 | Journal | J Med Chem | Structure-guided design of N-phenyl tertiary amines as transrepression-selective liver X receptor modulators with anti-inflammatory activity. | 18,800,767 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,754 | GW3965 | Synthetic organic | 6,435 | Agonist | Agonist | false | 135,650,333 | null | 7.52 | pEC50 | 10,546 | Journal | J Med Chem | Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines. | 11,985,463 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 10,034 | IMB-808 | Synthetic organic | 85,440 | Agonist | Partial agonist | false | 375,973,222 | false | 6.28 | pEC50 | 35,889 | Journal | Mol Pharmacol | Identification of a Novel Liver X Receptor Agonist that Regulates the Expression of Key Cholesterol Homeostasis Genes with Distinct Pharmacological Characteristics. | 28,087,808 | null |
||
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,688 | L-783483 | Synthetic organic | 6,434 | Agonist | Agonist | false | 135,650,496 | null | 8.2 | pKd | 10,566 | Journal | Endocrinology | A novel liver X receptor agonist establishes species differences in the regulation of cholesterol 7alpha-hydroxylase (CYP7a). | 12,072,387 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 9,625 | rovazolac | Synthetic organic | 84,454 | Agonist | Agonist | false | 340,590,255 | false | 6 | pEC50 | 33,389 | Patent | null | Liver x receptor (lxr) modulators for the treatment of dermal diseases, disorders and conditions | null | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 8,692 | SR9238 | Synthetic organic | 82,627 | Antagonist | Inverse agonist | false | 252,166,892 | false | 7.37 | pIC50 | 29,190 | Journal | ACS Chem Biol | A liver-selective LXR inverse agonist that suppresses hepatic steatosis. | 23,237,488 | null | null |
|
89 | nhr | 1H. Liver X receptor-like receptors | 601 | Liver X receptor-β | 2,755 | T0901317 | Synthetic organic | 6,436 | Agonist | Agonist | false | 135,651,223 | null | 7.3 | pEC50 | 10,571 | Journal | Genes Dev | Role of LXRs in control of lipogenesis. | 11,090,131 | null | PMC317060 |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 607 | Constitutive androstane receptor | 2,760 | androstanol | Synthetic organic | 6,442 | Antagonist | Inverse agonist | false | 135,649,945 | null | 6.4 | pIC50 | 10,596 | Journal | Nature | Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. | 9,783,588 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,789 | ZK159222 | Synthetic organic | 6,464 | Antagonist | Antagonist | false | 135,651,362 | false | 7.5 | pIC50 | 10,674 | Journal | Bioorg Med Chem | Design and synthesis of potent vitamin D receptor antagonists with A-ring modifications: remarkable effects of 2alpha-methyl introduction on antagonistic activity. | 12,901,907 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,789 | ZK159222 | Synthetic organic | 6,464 | Antagonist | Antagonist | false | 135,651,362 | false | 7.5 | pIC50 | 15,317 | Journal | Chem Biol | Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions. | 11,094,341 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,788 | TEI-9647 | Synthetic organic | 6,463 | Antagonist | Antagonist | false | 135,651,240 | false | 8.2 | pIC50 | 25,142 | Journal | J Med Chem | Further synthetic and biological studies on vitamin D hormone antagonists based on C24-alkylation and C2alpha-functionalization of 25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones. | 17,125,259 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,780 | tacalcitol | Synthetic organic | 6,451 | Agonist | Agonist | false | 135,651,286 | false | 8.5 | pKd | 10,661 | Journal | J Bone Miner Res | Profile of ligand specificity of the vitamin D binding protein for 1 alpha,25-dihydroxyvitamin D3 and its analogs. | 7,976,510 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,777 | seocalcitol | Synthetic organic | 6,448 | Agonist | Agonist | false | 135,650,217 | false | 9.6 | pKd | 10,662 | Journal | Bone | Studies on two new vitamin D analogs, EB 1089 and KH 1060: effects on bone resorption and osteoclast recruitment in vitro. | 8,573,413 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,777 | seocalcitol | Synthetic organic | 6,448 | Agonist | Agonist | false | 135,650,217 | false | 9.6 | pKd | 15,316 | Journal | Biochem Pharmacol | EB1089: a new vitamin D analogue that inhibits the growth of breast cancer cells in vivo and in vitro. | 1,472,092 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,791 | paricalcitol | Metabolite | 6,461 | Agonist | Agonist | true | FDA (1998) | 135,651,536 | true | null | - | null | null | null | null | null | null | null |
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,784 | maxacalcitol | Synthetic organic | 6,455 | Agonist | Agonist | false | 135,651,387 | null | 8.21 | pEC50 | 10,668 | Journal | Bone | Effects of two new vitamin D3 derivatives, 22-oxa-1 alpha-25-dihydroxyvitamin D3 (OCT) and 2 beta-(3-hydroxypropoxy)-1 alpha, 25-dihydroxyvitamin D3 (ED-71), on bone metabolism in organ culture. | 8,443,002 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 611 | lithocholic acid | Metabolite | 6,460 | Agonist | Agonist | false | 135,651,505 | null | 5.1 | pKi | 10,672 | Journal | Science | Vitamin D receptor as an intestinal bile acid sensor. | 12,016,314 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,787 | LG190178 | Synthetic organic | 6,458 | Agonist | Agonist | false | 135,650,519 | null | 6.82 | pKi | 10,671 | Journal | Chem Biol | Novel nonsecosteroidal vitamin D mimics exert VDR-modulating activities with less calcium mobilization than 1,25-dihydroxyvitamin D3. | 10,322,128 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,775 | lexacalcitol | Synthetic organic | 6,447 | Agonist | Agonist | false | 135,650,456 | null | 10.1 | pKd | 10,662 | Journal | Bone | Studies on two new vitamin D analogs, EB 1089 and KH 1060: effects on bone resorption and osteoclast recruitment in vitro. | 8,573,413 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 7,747 | inecalcitol | Natural product | 80,307 | Agonist | Agonist | false | 223,366,080 | true | 9.28 | pKd | 25,543 | Journal | Cancer Res | Two novel 14-Epi-analogues of 1,25-dihydroxyvitamin D3 inhibit the growth of human breast cancer cells in vitro and in vivo. | 10,825,140 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,782 | gemini | Synthetic organic | 6,453 | Agonist | Agonist | false | 135,650,299 | null | 8.5 | pKd | 10,666 | Journal | Biochem Pharmacol | Novel Gemini analogs of 1alpha,25-dihydroxyvitamin D(3) with enhanced transcriptional activity. | 15,013,848 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,781 | falecalcitriol | Synthetic organic | 6,452 | Agonist | Agonist | false | 135,650,250 | false | 8.8 | pKd | 10,665 | Journal | Bioorg Med Chem | Synthesis and biological evaluations of A-ring isomers of 26,26,26,27,27,27-hexafluoro-1,25-dihydroxyvitamin D3. | 11,003,160 | null | null |
|
90 | nhr | 1I. Vitamin D receptor-like receptors | 605 | Vitamin D receptor | 2,785 | elocalcitol | Synthetic organic | 6,456 | Agonist | Agonist | false | 135,650,914 | null | 8.21 | pIC50 | 10,669 | Journal | Endocrinology | Cellular and molecular events associated with the bone-protecting activity of the noncalcemic vitamin D analog Ro-26-9228 in osteopenic rats. | 11,956,143 | null | null |