CP-293019 [Ligand Id: 977] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL66227 (CP-293019) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | In vitro binding affinity against human D2 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 5.48 | pKi | >3310 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
| ChEMBL | Inhibition of human dopamine D2 receptor | B | 5.48 | pKi | >3310 | 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 | In vitro binding affinity against human D3 dopamine receptor in CHO cells using [3H]spiperone | B | 5.7 | pKi | >2000 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
| ChEMBL | Inhibition of human dopamine D3 receptor | B | 5.7 | pKi | >2000 | 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] | ||||||||
| ChEMBL | In vitro binding affinity at human D4 dopamine receptor in CHO cells by [3H]spiperone displacement. | B | 8.47 | pKi | 3.4 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
| D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 9.5 | pKi | - | - | - | Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188] |
| 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 | 6.74 | pKi | 180 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 1A receptor in CHO cells | B | 6.74 | pIC50 | 180 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
| 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 | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | In vitro binding affinity against 5-hydroxytryptamine 2A receptor in CHO cells | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 725-730 [PMID:9871530] |
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]
