pimavanserin [Ligand Id: 8423] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2111101 (Pimavanserin, Pimavanserina, Pimavanserine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: APLNR | F | 5.46 | pIC50 | 3436.69 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 | F | 5.34 | pIC50 | 4549.68 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 | F | 5.49 | pIC50 | 3258.17 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5.36 | pIC50 | 4329.7 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35 | F | 5.25 | pIC50 | 5642.31 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 | F | 5.45 | pIC50 | 3540.17 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from postmortem human brain membrane homogenate 5-HT2A receptor incubated for 120 mins by microbeta liquid scintillation counter analysis | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| GtoPdb | Ki determined in membrane radioligand binding assay. | - | 9.3 | pKi | - | - | - |
J Pharmacol Exp Ther (2004) 310: 943-51 [PMID:15102927]; J Pharmacol Exp Ther (2007) 322: 862-70 [PMID:17519387] |
| ChEMBL | Inverse agonist activity at 5-HT2A receptor (unknown origin) | F | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor incubated for 120 mins by microbeta liquid scintillation counter analysis | B | 10.2 | pKi | 0.06 | nM | Ki | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| ChEMBL | Inverse agonist activity at human 5-HT2A receptor assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry analysis | F | 7.1 | pIC50 | 79.43 | nM | IC50 | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| ChEMBL | Inverse agonist activity at 5-HT2A receptor (unknown origin) expressed in mouse NIH3T3 cells using o-nitrophenyl-D-galacto pyranoside incubated for 120 hrs | F | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2022) 234: 114246-114246 [PMID:35279606] |
| ChEMBL | Antagonist activity at 5-HT2A receptor (unknown origin) expressed in CHO-K1 cells assessed as reduction in intracellular Ca2+ mobilization incubated for 15 mins by FLIPR assay | F | 7.56 | pIC50 | 27.3 | nM | IC50 | Eur J Med Chem (2022) 234: 114246-114246 [PMID:35279606] |
| ChEMBL | Antagonist activity at 5HT2A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin hydrochloride-induced calcium flux preincubated for 1 hr followed by serotonin hydrochloride addition by calcium 6 dye based FLIPR assay | F | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2020) 63: 4171-4182 [PMID:32285676] |
| ChEMBL | Inverse agonist activity at human 5-HT2A receptor expressed in cell membrane assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry analysis | F | 7.9 | pIC50 | 12.6 | nM | IC50 | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| ChEMBL | Inverse agonist activity at human postmortem human brain membrane 5-HT2A receptor assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry analysis | F | 7.9 | pIC50 | 12.59 | nM | IC50 | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| ChEMBL | Antagonist activity at human 5-HT2A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 30 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay | F | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
| ChEMBL | Inverse agonist activity at human prefrontal cortex 5-HT2A receptor assessed as increase in [35S]GTPgammaS binding by liquid scintillation spectrometry analysis | F | 8.3 | pIC50 | 5.01 | nM | IC50 | J Med Chem (2023) 66: 9057-9075 [PMID:37378639] |
| ChEMBL | Inverse agonist activity at human full-length 5-HT2A | B | 8.73 | pIC50 | 1.86 | nM | IC50 | RSC Med Chem (2021) 12: 1459-1475 [PMID:34671731] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inverse agonist activity at 5-HT2C receptor (unknown origin) | F | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2022) 65: 10755-10808 [PMID:35939391] |
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]
