SC 53116 [Ligand Id: 238] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL34291 (SC-53116) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | The ability to inhibit [3H]prazosin binding to Alpha-1 adrenergic receptor in rat whole brain | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding affinity to adrenergic beta-1 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Binding affinity to adrenergic beta-2 receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Compound was evaluated for Dopamine receptor D1 binding | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3073-3075 [PMID:15149647] |
| ChEMBL | Binding affinity to dopamine receptor D1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | The ability to inhibit [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Compound was evaluated for Dopamine receptor D2 binding | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3073-3075 [PMID:15149647] |
| ChEMBL | Binding affinity to dopamine receptor D2 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Affinity of compound towards Dopamine receptor D2 in rat striatum using [3H]spiperone as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 702-715 [PMID:12593651] |
| ChEMBL | The ability to inhibit [3H]domperidone binding to dopamine receptor D2 in rat striata | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| 5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
| ChEMBL | Compound was evaluated for 5-hydroxytryptamine 3 receptor binding | B | 6.82 | pKi | 152 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 3073-3075 [PMID:15149647] |
| 5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| ChEMBL | Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxytryptamine 3 receptor | B | 6.82 | pKi | 152 | nM | Ki | J Med Chem (2003) 46: 702-715 [PMID:12593651] |
| ChEMBL | Inhibition of [3H]GR-65630 binding to 5-hydroxytryptamine 3 receptor | B | 6.82 | pKi | 152 | nM | Ki | J Med Chem (1992) 35: 1486-1489 [PMID:1573641] |
| ChEMBL | Displacement of [3H]GR65630 from 5HT3 receptor in brain cortex from Wistar rat | B | 6.82 | pKi | 152 | nM | Ki | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Compound was tested for 5-hydroxytryptamine 3 receptor binding affinity | B | 6.82 | pKi | 152 | nM | Ki | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae | F | 7.7 | pEC50 | 19.95 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2477-2480 |
| 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288] | ||||||||
| GtoPdb | - | - | 8.1 | pKi | - | - | - | FEBS Lett (1996) 398: 19-25 [PMID:8946946] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay of racemate mixture | F | 7.18 | pEC50 | 66 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3073-3075 [PMID:15149647] |
| ChEMBL | Efficient 5-hydroxytryptamine 4 agonist in the rat tunica muscularis mucosae | F | 7.63 | pEC50 | 23.7 | nM | EC50 | J Med Chem (2003) 46: 319-344 [PMID:12540230] |
| ChEMBL | Compound was tested for agonist activity at the 5-hydroxytryptamine 4 receptor in the rat tunica muscularis mucosae (TMM) assay | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3073-3075 [PMID:15149647] |
| ChEMBL | Agonism at 5HT4 receptor in rat tunica muscularis mucosa | F | 7.78 | pEC50 | 16.5 | nM | EC50 | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
| Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528] | ||||||||
| ChEMBL | Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4 receptor | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2003) 46: 702-715 [PMID:12593651] |
| ChEMBL | Displacement of [3H]GR-113808 from 5HT4 receptor in guinea pig striatum | B | 8.28 | pKi | 5.2 | nM | Ki | J Med Chem (2006) 49: 1125-1139 [PMID:16451077] |
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]
