capsazepine [Ligand Id: 2461] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL391997 (Capsazepine) |
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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 33:
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]
