PNU109291 [Ligand Id: 3228] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL71838 (PNU-109291) |
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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 | 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] |
| ChEMBL | Displacement of PNU-86170 from human dopamine D2 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based | B | 6.62 | pKi | 241 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
| 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] |
| ChEMBL | Displacement of spiperone from human dopamine D4 receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based | B | 5.43 | pKi | 3704 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
| 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] |
| ChEMBL | Displacement of 8-OH-DPAT from human 5-HT1A receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based | B | 5.96 | pKi | 1092 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
| 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-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based | B | 5.24 | pKi | 5775 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
| 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] |
| ChEMBL | Displacement of [3H]serotonin from recombinant human 5-HT1D receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based | B | 9.05 | pKi | 0.9 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
| 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 | Displacement of ketanserin from human 5-HT2A receptor expressed in CHO cell membrane incubated for 1 hr by competitive radioligand binding assay based | B | 6.77 | pKi | 168 | nM | Ki | Eur J Med Chem (2021) 210: 113073-113073 [PMID:33310287] |
ChEMBL data shown on this page come from version 35:
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]
