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ChEMBL ligand: CHEMBL229429 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
ChEMBL | Displacement of [3H]prazosin from adrenergic alpha-1A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Displacement of [3H]prazosin from adrenergic alpha-1B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | Displacement of [3H]cholidine from adrenergic alpha2A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | Displacement of [3H]cholidine from adrenergic alpha-2B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | Displacement of [3H]cholidine from adrenergic alpha-2C receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
ChEMBL | Displacement of [125I]pindolol from adrenergic beta-1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
ChEMBL | Displacement of [125I]pindolol from adrenergic beta-2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
ChEMBL | Displacement of [3H]DADLE from delta opioid receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Displacement of [3H]SCH-23390 from dopamine D1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from dopamine D2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from dopamine D3 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Displacement of [3H]N-methylspiperone from dopamine D4 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
ChEMBL | Displacement of radiolabeled SKF-38393 from dopamine D5 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | Displacement of [3H]WIN-35428 from DAT | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Binding affinity to histamine H1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
ChEMBL | Binding affinity to from histamine H2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
ChEMBL | Binding affinity to histamine H3 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8] | ||||||||
ChEMBL | Binding affinity to histamine H4 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]bremazocine from kappa opioid receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu1 receptor/Metabotropic glutamate receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3772] [GtoPdb: 289] [UniProtKB: Q13255] | ||||||||
ChEMBL | Binding affinity at mGluR1 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu2 receptor/Metabotropic glutamate receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5137] [GtoPdb: 290] [UniProtKB: Q14416] | ||||||||
ChEMBL | Binding affinity at mGluR2 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu4 receptor/Metabotropic glutamate receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2736] [GtoPdb: 292] [UniProtKB: Q14833] | ||||||||
ChEMBL | Binding affinity at mGluR4 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu5 receptor/Metabotropic glutamate receptor 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2564] [GtoPdb: 293] [UniProtKB: P31424] | ||||||||
ChEMBL | Displacement of [3H]MPEP from mGluR5 in rat brain | B | 10.44 | pKi | 0.04 | nM | Ki | J Med Chem (2011) 54: 901-908 [PMID:21207959] |
GtoPdb | - | - | 10.44 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2007) 50: 3256-66 [PMID:17571866] |
ChEMBL | Displacement of [3H]MPEP from mGluR5 in rat brain membrane | B | 10.44 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu6 receptor/Metabotropic glutamate receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4573] [GtoPdb: 294] [UniProtKB: O15303] | ||||||||
ChEMBL | Binding affinity at mGluR6 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
mGlu8 receptor/Metabotropic glutamate receptor 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3228] [GtoPdb: 296] [UniProtKB: O00222] | ||||||||
ChEMBL | Binding affinity at mGluR8 | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from mu opioid receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Displacement of [3H]QNB from muscarinic M1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Displacement of [3H]QNB from muscarinic M2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Displacement of [3H]QNB from muscarinic M3 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Displacement of [3H]QNB from muscarinic M4 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Displacement of [3H]QNB from muscarinic M5 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | Displacement of [3H]nisoxitine from NET | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Displacement of [3H]8-OH-DPAT from 5HT1A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Displacement of [3H]GR-125743 from 5HT1B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Displacement of [3H]GR-125743 from 5HT1D receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
ChEMBL | Displacement of [3H]5-HT from 5HT1E receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
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 5HT2A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5HT2B receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT3E/5-HT3B/5-HT3A/5-HT3D/5-HT3C/Serotonin 3 (5-HT3) receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094132] [GtoPdb: 377, 374, 373, 376, 375] [UniProtKB: A5X5Y0, O95264, P46098, Q70Z44, Q8WXA8] | ||||||||
ChEMBL | Displacement of [3H]zacopride from 5HT3 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5HT5A receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5HT6 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Displacement of [3H]LSD from 5HT7 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Displacement of [3H]citalopram from SERT | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
ChEMBL | Binding affinity to sigma1 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2007) 50: 3256-3266 [PMID:17571866] |
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]