CP-226269 [Ligand Id: 973] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL77395
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/D(4) dopamine receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity towards human 5-hydroxytryptamine 1A receptor B 6.7 pKi 200 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity towards human Dopamine receptor D2 B 6.92 pKi 120 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D2 receptor/D(2) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay B 6.28 pEC50 527 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay B 7.26 pEC50 55 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D3 receptor/D(3) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity towards human Dopamine receptor D3 B 6.25 pKi 560 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D4 receptor/D(4) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Binding affinity towards human D4.4 receptor B 8.44 pKi 3.6 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL Effective concentration against human Dopamine receptor D4 B 7.49 pEC50 32 nM EC50 J Med Chem (2004) 47: 2348-2355 [PMID:15084133]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay B 7.49 pEC50 32 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
D4 receptor/D(4) dopamine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
GtoPdb - - 9.4 pKi - - - Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay B 7.44 pEC50 36 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
ChEMBL In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay B 7.66 pEC50 22 nM EC50 J Med Chem (2004) 47: 3853-3864 [PMID:15239663]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity towards human Opioid receptor kappa 1 B 6.52 pKi 300 nM Ki J Med Chem (2004) 47: 3853-3864 [PMID:15239663]

ChEMBL data shown on this page come from version 36:

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]