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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 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]