A-381393 [Ligand Id: 8441] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL127257 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Inhibition of alpha2A adrenergic receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Inhibition of alpha2C adrenergic receptor (unknown origin) | B | 5.72 | pKi | 1912 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Inhibition of human dopamine D1 receptor | B | 5.1 | pKi | >8000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Inhibition of human dopamine D2 (long) receptor (unknown origin) | B | 5.22 | pKi | >6000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Inhibition of human dopamine D3 receptor | B | 5.22 | pKi | >6000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| GtoPdb | - | - | 8.82 | pKi | 1.5 | nM | Ki | Neuropharmacology (2005) 49: 112-21 [PMID:15992586] |
| ChEMBL | In vitro binding affinity tested on HEK293 cells co-transfected with human D4.4 receptor using [3H]spiperone as a radioligand in FLIPR assay | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Inhibition of human dopamine D4 receptor | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | In vitro inhibitory concentration tested on human D4.4 receptor in HEK293 cells using FLIPR assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Inhibition of human dopamine D5 receptor | B | 5.1 | pKi | >8000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Inhibition of histamine H1 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT1A receptor (unknown origin) | B | 5.86 | pKi | 1365 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT1B receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT2 receptor (unknown origin) | B | 6.43 | pKi | 370 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT2C receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT6 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT7 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | Inhibition of sigma2 receptor (unknown origin) | B | 5.7 | pKi | >2000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
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]
