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 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]
