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 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]
