ML 10375 [Ligand Id: 249] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL155917 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]-BRL 43694 as radioligand in rat posterior cortex. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]-BRL 43694 as radioligand in rat posterior cortex. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| 5-HT4 receptor in Human [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| GtoPdb | - | - | 10 | pKi | - | - | - |
Br J Pharmacol (2004) 143: 549-60 [PMID:15466450]; J Neurochem (1998) 70: 2252-61 [PMID:9603189]; Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]; Br J Pharmacol (2000) 130: 527-38 [PMID:10821780] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand | B | 8.63 | pKi | 2.32 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | 5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum | F | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
| ChEMBL | 5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum | F | 7.96 | pIC50 | 11 | nM | IC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
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]
