capsazepine [Ligand Id: 2461] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL391997 (Capsazepine)
There should be some charts here, you may need to enable JavaScript!
  • TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
  • 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!
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
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.4 pIC50 3981.07 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL Inhibition of TRPM8 (unknown origin) B 4.74 pIC50 18000 nM IC50 Bioorg Med Chem (2013) 21: 6542-6553 [PMID:24055075]
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 4.3 pIC50 >50000 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 4.3 pIC50 50000 nM IC50 J Nat Prod (2014) 77: 285-297 [PMID:24484240]
ChEMBL Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of icilin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to icilin stimulation by Fluo-4 AM dye based fluorescence assay B 4.3 pIC50 >50000 nM IC50 J Nat Prod (2014) 77: 1831-1838 [PMID:25052206]
ChEMBL Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of menthol-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to menthol stimulation by Fluo-4 AM dye based fluorescence assay B 4.3 pIC50 50000 nM IC50 J Nat Prod (2014) 77: 1831-1838 [PMID:25052206]
GtoPdb - - 4.7 pIC50 18000 nM IC50 Br J Pharmacol (2004) 141: 737-45 [PMID:14757700]
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1]
ChEMBL Binding affinity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane using [3H]-RTX as radioligand. B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2004) 14: 3053-3056 [PMID:15149643]
ChEMBL Binding affinity towards cloned human vanilloid receptor subtype 1 in HEK293 cell membranes using [3H]RTX as radioligand B 6.92 pKi 120 nM Ki Bioorg Med Chem Lett (2004) 14: 531-534 [PMID:14698197]
ChEMBL Inhibition of TRPV1 (unknown origin) B 5.59 pIC50 2600 nM IC50 Bioorg Med Chem (2013) 21: 6542-6553 [PMID:24055075]
ChEMBL Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells F 6.38 pIC50 420 nM IC50 J Med Chem (2005) 48: 71-90 [PMID:15634002]
ChEMBL Inhibition of calcium influx evoked by capsaicin in human TRPV1 expressing cells by fluorescence assay F 6.48 pIC50 334 nM IC50 J Med Chem (2006) 49: 471-474 [PMID:16420034]
ChEMBL Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay F 6.49 pIC50 320 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay B 6.82 pIC50 150 nM IC50 J Nat Prod (2014) 77: 285-297 [PMID:24484240]
ChEMBL Antagonistic activity towards human vanilloid receptor subtype 1 expressed in HEK293 cell membrane, as inhibition of agonist-induced intracellular [Ca2+] levels. F 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2004) 14: 3053-3056 [PMID:15149643]
ChEMBL Functional antagonistic activity against human vanilloid receptor subtype 1 in HEK293 cell membranes was determined as inhibition of agonist-induced increases in intracellular [Ca2+] levels F 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2004) 14: 531-534 [PMID:14698197]
ChEMBL Inhibition of human transient receptor potential vanilloid 1 receptor (n=5) B 7.13 pIC50 74 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay F 7.16 pIC50 69 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to capsaicin stimulation by Fluo-4 AM dye based fluorescence assay B 7.17 pIC50 68 nM IC50 J Nat Prod (2014) 77: 1831-1838 [PMID:25052206]
ChEMBL Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1 B 7.25 pIC50 56.2 nM IC50 J Med Chem (2005) 48: 4663-4669 [PMID:16000002]
ChEMBL Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay F 7.28 pIC50 53 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
GtoPdb - - 7.4 pIC50 39 nM IC50 Br J Pharmacol (2001) 132: 1084-94 [PMID:11226139]
ChEMBL Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay F 7.41 pIC50 39 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assay B 8.3 pIC50 5 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assay B 8.4 pIC50 4 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assay B 8.52 pIC50 3 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL In vitro inhibition of anandamide activated human TRPV1 receptor in [Ca2+] influx assay B 8.52 pIC50 3 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL In vitro inhibition of PMA-activated human TRPV1 receptor in [Ca2+] influx assay B 8.52 pIC50 3 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL Antagonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium levels by fluorimetric assay F 5.6 pEC50 2511.89 nM EC50 Bioorg Med Chem (2010) 18: 3299-3306 [PMID:20381363]
TRPV1/Vanilloid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5102] [GtoPdb: 507] [UniProtKB: O35433]
ChEMBL In vitro binding affinity towards Rat Vanilloid receptor 1 (VR1) by [3H]RTX displacement. B 5.89 pKi 1300 nM Ki J Med Chem (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX B 5.89 pKi 1300 nM Ki Bioorg Med Chem Lett (2005) 15: 4136-4142 [PMID:16005215]
ChEMBL In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells B 5.89 pKi 1300 nM Ki Bioorg Med Chem Lett (2005) 15: 4143-4150 [PMID:15993063]
ChEMBL Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells B 5.89 pKi 1300 nM Ki Bioorg Med Chem Lett (2007) 17: 214-219 [PMID:17035013]
ChEMBL Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells B 5.89 pKi 1300 nM Ki J Med Chem (2008) 51: 57-67 [PMID:18072720]
ChEMBL Displacement of [3H]RTX from Vanilloid receptor in Rat spinal cord membranes B 5.92 pKi 1200 nM Ki J Med Chem (1996) 39: 3123-3131 [PMID:8759633]
ChEMBL Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of calcium uptake F 6.28 pKi 520 nM Ki Bioorg Med Chem Lett (2007) 17: 214-219 [PMID:17035013]
ChEMBL Antagonist activity towards rat TRPV1 expressed in CHO cells F 6.28 pKi 520 nM Ki Bioorg Med Chem Lett (2005) 15: 4143-4150 [PMID:15993063]
ChEMBL Inhibition of capsaicin-induced [Ca2+] uptake by Rat Vanilloid receptor 1 (VR1) expressing CHO cells B 6.28 pKi 520 nM Ki J Med Chem (2003) 46: 3116-3126 [PMID:12825950]
ChEMBL Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium 45 uptake F 6.28 pKi 520 nM Ki J Med Chem (2008) 51: 57-67 [PMID:18072720]
ChEMBL Antagonist activity for rat TRPV1 expressed in CHO cells F 6.28 pKi 520 nM Ki Bioorg Med Chem Lett (2005) 15: 4136-4142 [PMID:16005215]
ChEMBL Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay F 4.4 pIC50 >40000 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay F 4.52 pIC50 >30000 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay F 6.05 pIC50 887 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
ChEMBL Inhibition of rat transient receptor potential vanilloid 1 receptor (n=2) B 6.44 pIC50 365 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]
ChEMBL Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay F 6.66 pIC50 220 nM IC50 J Med Chem (2007) 50: 2589-2596 [PMID:17489570]
GtoPdb - - 6.7 pIC50 - - - Br J Pharmacol (2001) 132: 1084-94 [PMID:11226139]
ChEMBL Vanilloid receptor subtype 1 antagonist activity based on its ability to block capsaicin-induced (CAP) activation of the rat VR1 channel in a HEK293 cell line F 7.24 pIC50 58 nM IC50 Bioorg Med Chem Lett (2003) 13: 3611-3616 [PMID:14505681]
ChEMBL In vitro inhibition of acid activated rat TRPV1 receptor in [Ca2+] influx assay B 8.4 pIC50 4 nM IC50 J Med Chem (2005) 48: 1857-1872 [PMID:15771431]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]