ChEMBL ligand: CHEMBL229430 (Amg-517, AMG-517)
TRPV1/Vanilloid receptor in Human [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] TRPV1/Vanilloid receptor in Rat [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433] 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
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL	Activation Assay: The cDNA for human TRPV1 (hTRPV1) was isolated by reverse transcriptase-polymerase chain reaction (RT-PCR) from human small intestine poly A+ RNA supplied by Clontech (Palo Alto, Calif.) using primers designed surrounding the initiation and termination codons identical to the published sequences (Hayes et al. Pain 2000, 88, 205-215). The resulting cDNA PCR products were subcloned into pCIneo mammalian expression vector (Promega) and fully sequenced using fluorescent dye-terminator reagents (Prism, PerkinElmer Applied Biosystems Division) and a PerkinElmer Applied Biosystems Model 373 DNA sequencer or Model 310 genetic analyzer. Expression plasmids encoding the hTRPV1 cDNA were transfected into HEK293 cells using Lipofectamine. Forty-eight hours after transfection, the neomycin-resistant cells were selected with growth medium containing 800 ug/mL Geneticin (Life Technologies, formerly Gibco BRL). Surviving individual colonies were isolated and screened for TRPV1 activity.	B	7.7	pIC50	20	nM	IC50	US-8969325-B2. TRPV1 antagonists (2015)
ChEMBL	FLIPR Assay: The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2+]i) using the Fluorescence Imaging Plate Reader (FLIPR)TETRA. All compounds were tested over a 12-point one-third-log concentration range. Compound stocks, 10 mM, were prepared in DMSO, and diluted serially across a 384-well plate using a Bravo BenchCel workstation (Agilent Technologies, Santa Clara, Calif.). A stock concentration of capsaicin (10 mM) was made in DMSO, and diluted in D-PBS to a final concentration of 200 nM (4x). On the day prior to the experiment, recombinant HEK293 cells that stably express human TRPV1 were removed from tissue culture flasks and plated in growth medium into black-walled clear-bottom 384-well Biocoat poly-D-lysine assay plates (BD Biosciences, Bedford, Mass.) using a Multidrop dispenser (ThermoScientific, Waltham, Mass.). On the day of the experiment, growth medium was removed, and the no-wash FLIPR Calcium-4 dye.	B	7.7	pIC50	20	nM	IC50	US-8802711-B2. TRPV1 antagonists (2014)
ChEMBL	Activation Assay: The functional activity of compounds at the TRPV1 receptor was determined by measurement of intracellular Ca2+ levels ([Ca2]i) using the Fluorescence Imaging Plate Reader (FLIPR)TETRA. All compounds were tested over a 12-point one-third-log concentration range. Compound stocks, 10 mM, were prepared in DMSO, and diluted serially across a 384-well plate using a Bravo BenchCel workstation (Agilent Technologies, Santa Clara, Calif.). A stock concentration of capsaicin (10 mM) was made in DMSO, and diluted in D-PBS to a final concentration of 200 nM (4x). On the day prior to the experiment, recombinant HEK293 cells that stably express either human or rat TRPV1 (hTRPV1-3) were removed from tissue culture flasks and plated in growth medium into black-walled clear-bottom 384-well Biocoat poly-D-lysine assay plates (BD Biosciences, Bedford, Mass.) using a Multidrop dispenser (ThermoScientific, Waltham, Mass.). On the day of the experiment, growth medium was removed.	B	7.7	pIC50	20	nM	IC50	US-8796328-B2. TRPV1 antagonists (2014)
ChEMBL	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of heat-induced calcium influx	F	8.89	pIC50	1.3	nM	IC50	J Med Chem (2007) 50: 3515-3527 [PMID:17585750]
GtoPdb	-	-	9	pIC50	0.9	nM	IC50	J Med Chem (2010) 53: 3330-48 [PMID:20307063]
ChEMBL	Inhibition of human TRPV1	B	9.05	pIC50	0.9	nM	IC50	J Med Chem (2010) 53: 3330-3348 [PMID:20307063]
ChEMBL	Antagonist activity at TRPV1 (unknown origin)	B	9.05	pIC50	0.9	nM	IC50	Bioorg Med Chem (2022) 56: 116614-116614 [PMID:35033884]
ChEMBL	Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced calcium influx	F	9.1	pIC50	0.8	nM	IC50	J Med Chem (2008) 51: 2744-2757 [PMID:18386885]
ChEMBL	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	F	9.12	pIC50	0.76	nM	IC50	J Med Chem (2007) 50: 3515-3527 [PMID:17585750]
ChEMBL	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization	F	9.12	pIC50	0.76	nM	IC50	Bioorg Med Chem Lett (2008) 18: 1830-1834 [PMID:18299195]
ChEMBL	Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx	F	9.21	pIC50	0.62	nM	IC50	J Med Chem (2007) 50: 3515-3527 [PMID:17585750]
ChEMBL	Antagonist activity at human TRPV1 assessed as inhibition of low pH-induced calcium influx	F	9.22	pIC50	0.6	nM	IC50	J Med Chem (2008) 51: 2744-2757 [PMID:18386885]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL	Antagonist activity at rat TRPV1	B	9.05	pIC50	0.9	nM	IC50	J Med Chem (2021) 64: 14046-14128 [PMID:34591488]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of capsaicin induced calcium influx	F	9.05	pIC50	0.9	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6539-6545 [PMID:17937985]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilization	F	9.05	pIC50	0.9	nM	IC50	Bioorg Med Chem Lett (2008) 18: 1830-1834 [PMID:18299195]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	F	9.05	pIC50	0.9	nM	IC50	J Med Chem (2008) 51: 2744-2757 [PMID:18386885]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced 45Ca2+ influx by FLIPR assay	F	9.05	pIC50	0.9	nM	IC50	Bioorg Med Chem Lett (2008) 18: 5118-5122 [PMID:18722118]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	F	9.05	pIC50	0.9	nM	IC50	J Med Chem (2007) 50: 3515-3527 [PMID:17585750]
ChEMBL	Inhibition of rat TRPV1 expressed in CHO cells assessed as capsaicin-induced Ca2+ influx	B	9.05	pIC50	0.9	nM	IC50	J Med Chem (2007) 50: 3528-3539 [PMID:17585751]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx	F	9.3	pIC50	0.5	nM	IC50	J Med Chem (2007) 50: 3515-3527 [PMID:17585750]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced calcium influx	F	9.3	pIC50	0.5	nM	IC50	J Med Chem (2008) 51: 2744-2757 [PMID:18386885]
ChEMBL	Inhibition of rat TRPV1 expressed in CHO cells assessed as acid-induced Ca2+ influx	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2007) 50: 3528-3539 [PMID:17585751]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of pH 5 acid-induced 45Ca2+ influx by FLIPR assay	F	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem Lett (2008) 18: 5118-5122 [PMID:18722118]
ChEMBL	Antagonist activity at rat TRPV1 expressed in CHO cells assessed inhibition of acid induced calcium influx	F	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem Lett (2007) 17: 6539-6545 [PMID:17937985]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]