PNU109291 [Ligand Id: 3228] 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: CHEMBL71838 (PNU-109291)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor in Gorilla [GtoPdb: 3]
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL The compound was tested for CNS binding affinity towards Dopamine receptor D2 from cloned Human membranes. B 6.62 pKi 241 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL The compound was tested for CNS binding affinity towards Dopamine receptor D4 from cloned Human membranes. B 5.43 pKi >3704 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1A receptor from cloned Human membranes. B 5.96 pKi 1092 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]
Serotonin 1b (5-HT1b) receptor in Gorilla (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304408] [UniProtKB: Q9N2B7]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells B 5.24 pKi 5775 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]
5-HT1D receptor in Gorilla [GtoPdb: 3]
GtoPdb - - 9.1 pKi 0.9 nM Ki J Med Chem (1998) 41: 2180-3 [PMID:9632349]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1D receptor from cloned gorilla membranes expressed in cultured HEK 293 cells B 9.05 pKi 0.9 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting B 9.05 pKi 0.9 nM Ki J Med Chem (2008) 51: 3609-3616 [PMID:18507369]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 2A receptor from cloned Human membranes B 6.77 pKi 168 nM Ki J Med Chem (1998) 41: 2180-2183 [PMID:9632349]

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]