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] |
| ChEMBL | Binding affinity to human D2R assessed as inhibition constant | B | 5.48 | pKi | >3310 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| 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] |
| ChEMBL | Binding affinity to human D4R assessed as inhibition constant | B | 8.47 | pKi | 3.4 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| 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 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]
