ChEMBL ligand: CHEMBL294199 (ALGRX 4975, ALGRX-4975, Ausanil, Axsain, Capsaicin, Capzasin-hp, Cntx-4975, Dolenon, FEMA NO. 3404, Mioton, Ngx-1998, NGX-1998, NGX-4010, NSC-56353, Ovocap, Qutenza, Ratden pe 40, Togarashi orenji, Trans-capsaicin, Zacin, Zostrix, Zostrix hp)
5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] There should be some charts here, you may need to enable JavaScript!
CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] There should be some charts here, you may need to enable JavaScript!
CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] There should be some charts here, you may need to enable JavaScript!
COX-1 /Cyclooxygenase-1 in Human [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] There should be some charts here, you may need to enable JavaScript!
CYP1A2/Cytochrome P450 1A2 in Human [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177] There should be some charts here, you may need to enable JavaScript!
NADH-ubiquinone oxidoreductase chain 1 in Bovine [ChEMBL: CHEMBL4497] [UniProtKB: P03887] There should be some charts here, you may need to enable JavaScript!
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5] There should be some charts here, you may need to enable JavaScript!
Tyrosyl-tRNA synthetase in Human [ChEMBL: CHEMBL3179] [UniProtKB: P54577] There should be some charts here, you may need to enable JavaScript!
TRPV1/Vanilloid receptor in Human [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3] TRPV1/Vanilloid receptor in Rat [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] There should be some charts here, you may need to enable JavaScript!
Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470] Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388] There should be some charts here, you may need to enable JavaScript!
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142] There should be some charts here, you may need to enable JavaScript!
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2] There should be some charts here, you may need to enable JavaScript!
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL	Inhibition of human PMNL 5-LOX using arachidonic acid as substrate after 5 mins by HPLC method	B	4.25	pIC50	56000	nM	IC50	Bioorg Med Chem (2019) 27: 3745-3759 [PMID:31331653]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cell membrane	B	5	pKi	>10000	nM	Ki	J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
ChEMBL	Displacement of [3H]-CP55940 from human recombinant cannabinoid CB1 receptor expressed in HEK cells by Cheng-Prusoff analysis	B	5.25	pKi	>5600	nM	Ki	J Med Chem (2020) 63: 12290-12358 [PMID:32686940]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cell membrane	B	5	pKi	>10000	nM	Ki	J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL	Inhibition of COX1	B	5.42	pIC50	3800	nM	IC50	J. Nat. Prod. (2005) 68: 985-991 [PMID:16038536]
ChEMBL	DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)	B	5.81	pIC50	1551	nM	IC50	DrugMatrix in vitro pharmacology data
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL	DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin)	B	5.52	pIC50	3000	nM	IC50	DrugMatrix in vitro pharmacology data
NADH-ubiquinone oxidoreductase chain 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4497] [UniProtKB: P03887]
ChEMBL	Inhibition of Bos taurus (bovine) heart submitochondrial particle NDH1 assessed as NADH-DB reductase activity	B	4.28	pIC50	52480.75	nM	IC50	Biochim. Biophys. Acta (1996) 1273: 21-30 [PMID:8573592]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108632] [GtoPdb: 500] [UniProtKB: Q8R4D5]
ChEMBL	Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx by fluorescence-based assay	B	4	pIC50	>100000	nM	IC50	J. Nat. Prod. (2014) 77: 285-297 [PMID:24484240]
ChEMBL	Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of menthol-induced intracellular Ca2+ influx by fluorescence-based assay	B	4.55	pIC50	28000	nM	IC50	J. Nat. Prod. (2014) 77: 285-297 [PMID:24484240]
Tyrosyl-tRNA synthetase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3179] [UniProtKB: P54577]
ChEMBL	Compound was tested for the inhibition of aminoacyl tRNA Synthetase	B	4.38	pKi	42000	nM	Ki	Bioorg. Med. Chem. Lett. (1997) 7: 2363-2366
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL	Displacement of [3H]MPOU from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method	B	5.6	pKi	2530	nM	Ki	J Med Chem (2017) 60: 8246-8252 [PMID:28892388]
ChEMBL	Displacement of [3H]RTX from human TRPV1 expressed in CHO cell membranes after 45 mins by scintillation counting method	B	5.94	pKi	1140	nM	Ki	J Med Chem (2017) 60: 8246-8252 [PMID:28892388]
ChEMBL	Displacement of [3H]-RTX from human TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting method	B	5.97	pKi	1070	nM	Ki	J Med Chem (2020) 63: 418-424 [PMID:31702924]
ChEMBL	Binding affinity to human recombinant TRPV1	B	8.22	pKi	6	nM	Ki	Bioorg. Med. Chem. Lett. (2010) 20: 7137-7141 [PMID:20947352]
ChEMBL	Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin-induced Ca2+ influx pre-treated 5 mins before capsaicin addition by Fluo-4 dye based assay	B	8.1	pIC50	8	nM	IC50	Bioorg. Med. Chem. Lett. (2015) 25: 1009-1011 [PMID:25666822]
ChEMBL	Antagonist activity at human TRPV1 stably transfected in HEK293 cells assessed as decrease in calcium influx preincubated for 5 mins followed by capsaicin addition by Fluo-4-AM dye based spectrofluorimetric method	B	8.1	pIC50	8	nM	IC50	J Nat Prod (2020) 83: 3476-3481 [PMID:33136399]
ChEMBL	Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as effect on intracellular calcium level by FLOU-4 dye based fluorescence spectrometry	B	4.52	pEC50	30200	nM	EC50	J Med Chem (2020) 63: 12290-12358 [PMID:32686940]
ChEMBL	Agonist activity at TRPV1 (unknown origin) expressed in human SH-SY5Y cells assessed as increase in calcium influx after 25 mins by Fluo-4 NW dye-based fluorescence assay	B	6	pEC50	1000	nM	EC50	J Med Chem (2018) 61: 4436-4455 [PMID:29722529]
ChEMBL	Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followed by compound washout via perfusion for 1 min by FURA-2AM-dye based fluorescence assay	B	6.06	pEC50	870.96	nM	EC50	J Med Chem (2018) 61: 3126-3137 [PMID:29543451]
ChEMBL	Agonist activity at recombinant TRPV1 (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux administered for 1 min followed by compound washout via perfusion for 1 min by FURA-2AM-dye based fluorescence assay	B	6.06	pEC50	870	nM	EC50	J Med Chem (2018) 61: 3126-3137 [PMID:29543451]
ChEMBL	Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation of calcium uptake by 45Ca2+ uptake assay	B	7.35	pEC50	44.8	nM	EC50	J Med Chem (2021) 64: 370-384 [PMID:33385210]
ChEMBL	Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells	F	7.4	pEC50	40	nM	EC50	Bioorg. Med. Chem. Lett. (2007) 17: 132-135 [PMID:17046253]
ChEMBL	Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level	F	7.4	pEC50	40	nM	EC50	Bioorg. Med. Chem. Lett. (2010) 20: 97-99 [PMID:19951840]
GtoPdb	-	-	7.5	pEC50	31.6	nM	EC50	Nature (2004) 430: 748-54 [PMID:15306801]
ChEMBL	Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method	B	7.59	pEC50	25.9	nM	EC50	J Med Chem (2020) 63: 418-424 [PMID:31702924]
ChEMBL	Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as increase in intracellular calcium level	F	7.7	pEC50	20	nM	EC50	J. Med. Chem. (2009) 52: 3001-3009 [PMID:19361197]
ChEMBL	Concentration necessary to induce a relative half-maximal response measured by the entry of [Ca2+] into human embryonic kidney HEK293 cells overexpressing the human VR1	F	7.7	pEC50	19.95	nM	EC50	J. Med. Chem. (2002) 45: 3739-3745 [PMID:12166946]
ChEMBL	Agonist activity at human TRPV1 expressed in HEK293T cells assessed as increase in Ca2+ transport incubated for 5 mins by calcium-5 fluorescence dye-based FLIPR assay	B	8.14	pEC50	7.2	nM	EC50	Bioorg Med Chem (2019) 27: 2893-2904 [PMID:31104785]
ChEMBL	Agonist activity at human TRPV1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method	B	8.28	pEC50	5.3	nM	EC50	J Nat Prod (2020) 83: 3476-3481 [PMID:33136399]
ChEMBL	Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as Ca2+ influx by Fluo-4 dye based assay	B	8.28	pEC50	5.3	nM	EC50	Bioorg. Med. Chem. Lett. (2015) 25: 1009-1011 [PMID:25666822]
ChEMBL	Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed as calcium influx by fluo-4-Am-based fluorimetry	F	8.41	pEC50	3.9	nM	EC50	Bioorg. Med. Chem. Lett. (2012) 22: 1674-1677 [PMID:22257892]
ChEMBL	Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as increase in intracellular calcium levels by fluorimetric assay	F	8.6	pEC50	2.51	nM	EC50	Bioorg. Med. Chem. (2010) 18: 3299-3306 [PMID:20381363]
TRPV1 in Mouse [GtoPdb: 507] [UniProtKB: Q704Y3]
GtoPdb	-	-	8	pEC50	-	-	-	Neurosci Lett (2004) 370: 55-60 [PMID:15489017]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL	Binding affinity against Vanilloid receptor in dorsal Root Ganglion (DRG) membranes using [3H]RTX binding assay.	B	5.7	pKi	2000	nM	Ki	J. Med. Chem. (1996) 39: 2939-2952 [PMID:8709128]
ChEMBL	Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranes	B	5.7	pKi	2000	nM	Ki	J. Med. Chem. (1996) 39: 3123-3131 [PMID:8759633]
ChEMBL	Displacement of [3H]-RTX from rat TRPV1 expressed in CHO cells incubated for 60 mins by radioligand competition assay based scintillation counting method	B	5.74	pKi	1810	nM	Ki	J Med Chem (2020) 63: 418-424 [PMID:31702924]
ChEMBL	Displacement of [3H]RTX form rat TRPV1 receptor expressed in CHO/VR1 cell system	B	5.74	pKi	1808	nM	Ki	Bioorg. Med. Chem. (2009) 17: 690-698 [PMID:19135377]
ChEMBL	In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]RTX displacement.	B	5.74	pKi	1800	nM	Ki	J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL	In vitro binding to Rat Vanilloid receptor 1 (VR1) expressing CHO cells compared to capsaicin	B	5.77	pKi	1700	nM	Ki	J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL	Binding affinity to rat TRPV1	B	7.72	pIC50	19	nM	IC50	Bioorg. Med. Chem. Lett. (2010) 20: 7137-7141 [PMID:20947352]
ChEMBL	Agonist activity at rat TRPV1 expressed in human SH-SY5Y cells assessed as intracellular calcium accumulation by Fluo-4 NW dye based fluorescence assay	B	5.63	pEC50	2320	nM	EC50	ACS Med Chem Lett (2019) 10: 143-144 [PMID:30783490]
GtoPdb	-	-	6.1	pEC50	-	-	-	Nature (1997) 389: 816-24 [PMID:9349813]
ChEMBL	In vitro [Ca2+] influx relative to capsaicin by Rat Vanilloid receptor (VR1) expressing CHO cells	F	7.35	pEC50	44.8	nM	EC50	J. Med. Chem. (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL	Agonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium uptake	F	7.35	pEC50	44.8	nM	EC50	Bioorg. Med. Chem. (2009) 17: 690-698 [PMID:19135377]
ChEMBL	Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45Ca2+ uptake incubated for 5 mins by liquid scintillation counting method	B	7.35	pEC50	44.8	nM	EC50	J Med Chem (2020) 63: 418-424 [PMID:31702924]
Kv1.1/Voltage-gated potassium channel subunit Kv1.1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2309] [GtoPdb: 538] [UniProtKB: Q09470]
ChEMBL	Inhibition of Kv1.1 (unknown origin)	B	4.54	pIC50	29000	nM	IC50	J Med Chem (2017) 60: 2245-2256 [PMID:28225274]
Kv1.1 in Mouse [GtoPdb: 538] [UniProtKB: P16388]
GtoPdb	-	-	4.5	pIC50	-	-	-	Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.2 in Rat [GtoPdb: 539] [UniProtKB: P63142]
GtoPdb	-	-	4.4	pKd	45000	nM	Kd	Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]
Kv1.7 in Mouse [GtoPdb: 544] [UniProtKB: Q17ST2]
GtoPdb	-	-	4.6	pIC50	-	-	-	J Biol Chem (1998) 273: 5851-7 [PMID:9488722]
Kv3.1 in Mouse [GtoPdb: 548] [UniProtKB: P15388]
GtoPdb	-	-	3.8	pIC50	-	-	-	Mol Pharmacol (1994) 45: 1227-34 [PMID:7517498]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]