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

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ChEMBL ligand: CHEMBL391997 (Capsazepine)
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  • 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]
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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 28:

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]