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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,397 | bupivacaine | Synthetic organic | 84,594 | Channel blocker | Pore blocker | true | FDA (1972), EMA (2020) | 135,650,032 | false | 4.16 | pIC50 | 33,683 | Journal | Anesth Analg | A Comparative Analysis of Bupivacaine and Ropivacaine Effects on Human Cardiac SCN5A Channels. | 25,692,452 | null | null |
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,615 | Bc-III | Peptide | 6,233 | Gating inhibitor | Slows inactivation | false | 135,652,013 | false | 6.5 | pEC50 | 9,819 | Journal | J Biol Chem | Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop. | 15,169,781 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,619 | batrachotoxin | Natural product | 6,232 | Activator | Full agonist | false | 135,652,668 | false | 7.6 | pKd | 9,937 | Journal | Mol Pharmacol | Binding of [3H]batrachotoxinin A benzoate to specific sites on rat cardiac sodium channels. | 2,431,264 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,614 | ATX-II | Peptide | 6,231 | Gating inhibitor | Slows inactivation | false | 135,652,003 | false | 7.3 | pEC50 | 9,819 | Journal | J Biol Chem | Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop. | 15,169,781 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,566 | amiodarone | Synthetic organic | 6,230 | Channel blocker | Pore blocker | true | FDA (1985) | 135,649,937 | false | 5.7 | pIC50 | 9,936 | Journal | Circ Res | Amiodarone: biochemical evidence for binding to a receptor for class I drugs associated with the rat cardiac sodium channel. | 2,546,697 | null | null |
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 10,119 | AM-6120 | Peptide | 85,664 | Inhibitor | Inhibition | false | 381,118,829 | false | 5.18 | pIC50 | 36,313 | Journal | J Med Chem | Discovery of Tarantula Venom-Derived Na<sub>V</sub>1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis. | 30,346,167 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,618 | α-scorpion toxin 2 | Peptide | 6,229 | Gating inhibitor | Slows inactivation | false | 135,651,986 | false | 7.7 | pKd | 9,842 | Journal | J Biol Chem | Molecular determinants of high affinity binding of alpha-scorpion toxin and sea anemone toxin in the S3-S4 extracellular loop in domain IV of the Na+ channel alpha subunit. | 8,663,157 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,613 | AFT-II | Peptide | 6,228 | Gating inhibitor | Slows inactivation | false | 135,651,976 | false | 7.2 | pEC50 | 9,819 | Journal | J Biol Chem | Binding specificity of sea anemone toxins to Nav 1.1-1.6 sodium channels: unexpected contributions from differences in the IV/S3-S4 outer loop. | 15,169,781 | null | null |
|
82 | vgic | Voltage-gated sodium channels (Na<sub>V</sub>) | 582 | Na<sub>v</sub>1.5 | 2,617 | aconitine | Natural product | 6,227 | Activator | Partial agonist | false | 135,652,663 | false | null | - | 9,935 | Journal | Gen Physiol Biophys | Properties of aconitine-modified sodium channels in single cells of mouse ventricular myocardium. | 2,433,183 | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,176 | diBA-(5)-C4 | Synthetic organic | 12,328 | Channel blocker | None | null | null | 178,100,995 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,100 | 1,9-dideoxyforskolin | Natural product | 12,209 | Channel blocker | None | false | 178,100,923 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,113 | 9-anthroic acid | Synthetic organic | 12,232 | Channel blocker | None | false | 178,100,935 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 2,391 | arachidonic acid | Metabolite | 11,775 | Channel blocker | None | false | 135,651,442 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,151 | carbenoxolone | Synthetic organic | 12,277 | Channel blocker | None | false | 178,100,972 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,159 | clomiphene | Synthetic organic | 12,305 | Channel blocker | None | true | FDA (1967) | 178,100,979 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,174 | DCPIB | Synthetic organic | 12,327 | Channel blocker | None | false | 178,100,994 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 1,016 | tamoxifen | Synthetic organic | 11,651 | Channel blocker | None | true | FDA (1977) | 135,651,233 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 2,510 | quinine | Natural product | 11,989 | Channel blocker | None | true | FDA (2005, as quinine sulfate, previous history unspecified) | 135,652,709 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 2,342 | quinidine | Natural product | 11,716 | Channel blocker | None | true | FDA (1950) | 135,650,872 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,273 | NS3728 | Synthetic organic | 12,454 | Channel blocker | None | false | 178,101,090 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,270 | NPPB | Synthetic organic | 11,256 | Channel blocker | None | false | 178,101,087 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,265 | nordihydroguiaretic acid | Natural product | 12,441 | Channel blocker | None | true | FDA (1992) | 178,101,082 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,263 | nafoxidine | Synthetic organic | 12,440 | Channel blocker | None | null | null | 178,101,080 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 2,522 | mibefradil | Synthetic organic | 12,003 | Channel blocker | None | true | FDA (1997) | 53,801,058 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 708 | Mg<sup>2+</sup> | Inorganic | 11,645 | Channel blocker | None | false | 135,652,741 | false | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,252 | mefloquine | Synthetic organic | 12,421 | Channel blocker | None | true | FDA (1989), UK (1989) | 178,101,069 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,217 | IAA-94 | Synthetic organic | 12,370 | Channel blocker | None | false | 178,101,034 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,207 | GTPγS | Synthetic organic | 12,355 | Activator | None | null | null | 178,101,024 | null | null | - | null | null | null | null | null | null | null |
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,204 | gossypol | Natural product | 12,350 | Channel blocker | None | false | 178,101,021 | null | null | - | null | null | null | null | null | null | null |
|
132 | other_ic | Volume regulated chloride channels (VRAC) | 710 | VRAC | 4,177 | DIDS | Synthetic organic | 11,252 | Channel blocker | None | false | 178,100,996 | null | null | - | null | null | null | null | null | null | null |
|
157 | transporter | V-type ATPase | 812 | V-type ATPase V<sub>1</sub> motor B2 subunit | 8,882 | enoxacin | Synthetic organic | 82,997 | Inhibitor | Inhibition | true | FDA (1991) | 252,827,539 | false | 5 | pIC50 | 30,022 | Journal | J Med Chem | Identification of enoxacin as an inhibitor of osteoclast formation and bone resorption by structure-based virtual screening. | 19,630,402 | null | PMC2889180 |
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 13,061 | compound 22 [PMID: 38085679] | Synthetic organic | 90,207 | Inhibitor | Inhibition | false | 491,299,843 | false | 10.7 | pKi | 46,464 | Journal | J Med Chem | Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors. | 38,085,679 | null | null |
|
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 11,999 | compound 41 [PMID: 35436124] | Synthetic organic | 88,679 | Inhibitor | Binding | false | 464,244,140 | false | 10.7 | pKi | 43,696 | Journal | J Med Chem | Discovery of Potent Orally Bioavailable WD Repeat Domain 5 (WDR5) Inhibitors Using a Pharmacophore-Based Optimization. | 35,436,124 | null |
||
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 13,043 | MS132 | Synthetic organic | 90,187 | None | Binding | false | 491,299,825 | false | 6.91 | pKd | 46,410 | Journal | J Med Chem | Discovery of Potent and Selective WDR5 Proteolysis Targeting Chimeras as Potential Therapeutics for Pancreatic Cancer. | 38,019,706 | null | PMC10872723 |
|
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 12,000 | MS40 | Synthetic organic | 88,680 | Inhibitor | Binding | false | 464,244,141 | false | 6.9 | pKd | 43,702 | Journal | Oncogene | Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic. | 35,525,905 | null | PMC9189076 |
|
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 8,231 | OICR-9429 | Synthetic organic | 81,844 | Inhibitor | Binding | false | 249,565,911 | true | 7.62 | pKd | 27,120 | Webpage | null | OICR-9429 - a chemical probe for WDR5. | null | null |
||
903 | other_protein | WD repeat-containing proteins | 2,831 | WD repeat domain 5 | 8,231 | OICR-9429 | Synthetic organic | 81,844 | Inhibitor | Binding | false | 249,565,911 | true | 7.62 | pKd | 43,703 | Journal | Nat Chem Biol | Erratum: Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia. | 26,379,026 | null |
||
642 | enzyme | WEE family | 2,278 | WEE1 G2 checkpoint kinase | 7,702 | adavosertib | Synthetic organic | 80,186 | Inhibitor | Inhibition | false | 223,366,035 | true | 8.29 | pIC50 | 25,398 | Webpage | null | AZD1775. | null | null |
||
642 | enzyme | WEE family | 2,167 | protein kinase, membrane associated tyrosine/threonine 1 | 8,183 | PD166285 | Synthetic organic | 81,702 | Inhibitor | Inhibition | false | 249,565,863 | false | null | pIC50 | 26,989 | Journal | Cancer Res | Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. | 11,719,452 | null | null |
|
642 | enzyme | WEE family | 2,167 | protein kinase, membrane associated tyrosine/threonine 1 | 8,183 | PD166285 | Synthetic organic | 81,702 | Inhibitor | Inhibition | false | 249,565,863 | false | null | pIC50 | 26,990 | Journal | Bioorg Med Chem Lett | In vitro and in silico studies on substrate recognition and acceptance of human PKMYT1, a Cdk1 inhibitory kinase. | 22,189,141 | null | null |
|
642 | enzyme | WEE family | 2,278 | WEE1 G2 checkpoint kinase | 11,731 | azenosertib | Synthetic organic | 88,291 | Inhibitor | Inhibition | false | 458,923,766 | false | 8.41 | pIC50 | 42,985 | Journal | J Med Chem | Discovery of ZN-c3, a Highly Potent and Selective Wee1 Inhibitor Undergoing Evaluation in Clinical Trials for the Treatment of Cancer. | 34,423,975 | null |
||
642 | enzyme | WEE family | 2,278 | WEE1 G2 checkpoint kinase | 8,183 | PD166285 | Synthetic organic | 81,701 | Inhibitor | Inhibition | false | 249,565,863 | false | 7.62 | pIC50 | 26,989 | Journal | Cancer Res | Radiosensitization of p53 mutant cells by PD0166285, a novel G(2) checkpoint abrogator. | 11,719,452 | null | null |
|
642 | enzyme | WEE family | 2,167 | protein kinase, membrane associated tyrosine/threonine 1 | 12,072 | (S)-RP-6306 | Synthetic organic | 88,784 | Inhibitor | Inhibition | false | 472,319,194 | false | 8.7 | pIC50 | 43,920 | Journal | J Med Chem | Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. | 35,880,755 | null | PMC9837800 |
|
643 | enzyme | Wnk family | 2,280 | WNK lysine deficient protein kinase 1 | 8,836 | PP1 | Synthetic organic | 82,879 | Inhibitor | Inhibition | false | 252,827,493 | false | 4.9 | pKi | 29,919 | Journal | Biochemistry | Kinetic mechanism and inhibitor characterization of WNK1 kinase. | 19,739,668 | null | null |
|
643 | enzyme | Wnk family | 2,281 | WNK lysine deficient protein kinase 2 | 8,122 | compound 25 [PMID: 17935989] | Synthetic organic | 82,776 | Inhibitor | Inhibition | false | 249,565,802 | false | 5.82 | pKi | 26,906 | Journal | Bioorg Med Chem Lett | Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. | 17,935,989 | null | null |
|
643 | enzyme | Wnk family | 2,282 | WNK lysine deficient protein kinase 3 | 8,138 | compound 2c [PMID: 24900538] | Synthetic organic | 81,748 | Inhibitor | Inhibition | false | 249,565,818 | false | 7 | pIC50 | 26,922 | Journal | ACS Med Chem Lett | Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors. | 24,900,538 | null | PMC4025776 |
|
644 | enzyme | YANK family | 1,538 | serine/threonine kinase 32B | 8,219 | compound 74 [PMID: 24793884] | Synthetic organic | 81,820 | Inhibitor | Inhibition | false | 249,565,899 | false | null | - | 27,038 | Journal | Eur J Med Chem | Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. | 24,793,884 | null | null |
|
552 | enzyme | YSK subfamily | 2,217 | serine/threonine kinase 24 | 5,710 | bosutinib | Synthetic organic | 81,653 | Inhibitor | Inhibition | true | FDA (2012), EMA (2013) | 178,102,336 | false | 8.41 | pIC50 | 23,854 | Journal | Leukemia | Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells. | 19,039,322 | null | null |
83 | lgic | ZAC | 587 | ZAC | 566 | Zn<sup>2+</sup> | Inorganic | 11,278 | Agonist | Agonist | false | 135,652,747 | false | null | pEC50 | 31,280 | Journal | Biochem Pharmacol | Copper and protons directly activate the zinc-activated channel. | 26,872,532 | null | PMC5119521 |
|
83 | lgic | ZAC | 587 | ZAC | 566 | Zn<sup>2+</sup> | Inorganic | 11,278 | Agonist | Agonist | false | 135,652,747 | false | null | pEC50 | 7,525 | Journal | J Biol Chem | A novel class of ligand-gated ion channel is activated by Zn2+. | 12,381,728 | null | null |
|
83 | lgic | ZAC | 587 | ZAC | 2,294 | tubocurarine | Natural product | 11,291 | Antagonist | Antagonist | true | FDA (1945) | 135,652,723 | false | 5.2 | pIC50 | 7,525 | Journal | J Biol Chem | A novel class of ligand-gated ion channel is activated by Zn2+. | 12,381,728 | null | null |
83 | lgic | ZAC | 587 | ZAC | 12,563 | TTFB | Synthetic organic | 89,577 | Allosteric modulator | Antagonist | false | 479,821,353 | false | 5.5 | pIC50 | 45,231 | Journal | Biochem Pharmacol | Discovery and functional characterization of N-(thiazol-2-yl)-benzamide analogs as the first class of selective antagonists of the Zinc-Activated Channel (ZAC). | 34,560,054 | null |
||
83 | lgic | ZAC | 587 | ZAC | 2,346 | H<sup>+</sup> | Inorganic | 83,700 | Agonist | Agonist | false | 135,652,738 | false | 5.6 | pEC50 | 31,280 | Journal | Biochem Pharmacol | Copper and protons directly activate the zinc-activated channel. | 26,872,532 | null | PMC5119521 |
|
83 | lgic | ZAC | 587 | ZAC | 4,164 | Cu<sup>2+</sup> | Inorganic | 83,701 | Agonist | Agonist | false | 178,100,984 | false | 5.4 | pEC50 | 31,280 | Journal | Biochem Pharmacol | Copper and protons directly activate the zinc-activated channel. | 26,872,532 | null | PMC5119521 |
|
83 | lgic | ZAC | 587 | ZAC | 707 | Ca<sup>2+</sup> | Inorganic | 83,702 | Antagonist | Antagonist | false | 135,652,731 | false | 2.03 | pIC50 | 31,280 | Journal | Biochem Pharmacol | Copper and protons directly activate the zinc-activated channel. | 26,872,532 | null | PMC5119521 |