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ChEMBL ligand: CHEMBL522460 |
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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 | Binding affinity to human adrenergic alpha1A receptor by radioligand displacement assay | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
ChEMBL | Binding affinity to human adrenergic Alpha-1B receptor by radioligand displacement assay | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
ChEMBL | Binding affinity to human adrenergic Alpha-1D receptor by radioligand displacement assay | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Antagonist activity at dopamine D2 receptor | F | 5.29 | pIC50 | 5100 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Inhibition of dopamine D2 receptor | B | 5.58 | pIC50 | 2650 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
ChEMBL | Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at muscarinic M1 receptor | F | 6.54 | pEC50 | 289 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Agonist activity at muscarinic M1 receptor | F | 6.54 | pEC50 | 289 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
ChEMBL | Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response | F | 6.59 | pEC50 | 257.04 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at human muscarinic M1 receptor expressed in CHO cells calcium response | F | 6.59 | pEC50 | 255 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay | F | 8.19 | pEC50 | 6.5 | nM | EC50 | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
ChEMBL | Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs | B | 6.22 | pKi | 602.56 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs | B | 6.22 | pKi | 600 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response | F | 7.1 | pEC50 | 79.6 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M1 receptor expressed in CHO cells calcium response | F | 7.1 | pEC50 | 79.43 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
ChEMBL | Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells | B | 6.49 | pKi | 320 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.46 | pIC50 | 3500 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at human muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.46 | pIC50 | 3467.37 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at muscarinic M2 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Agonist activity at muscarinic M2 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
ChEMBL | Partial agonist activity at human muscarinic M2 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
ChEMBL | Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.89 | pIC50 | 1290 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at rat muscarinic M2 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.89 | pIC50 | 1288.25 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M2 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells | B | 6.37 | pKi | 430 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.63 | pIC50 | 2344.23 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at human muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.64 | pIC50 | 2300 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at muscarinic M3 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Agonist activity at muscarinic M3 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
ChEMBL | Partial agonist activity at human muscarinic M3 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
ChEMBL | Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.26 | pIC50 | 5495.41 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at rat muscarinic M3 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.26 | pIC50 | 5480 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M3 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 6.13 | pIC50 | 741.31 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at human muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 6.13 | pIC50 | 734 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at muscarinic M4 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Agonist activity at muscarinic M4 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
ChEMBL | Partial agonist activity at human muscarinic M4 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
ChEMBL | Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 6.31 | pIC50 | 493 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at rat muscarinic M4 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 6.31 | pIC50 | 489.78 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M5 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Partial agonist activity at rat muscarinic M4 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells | B | 6.03 | pKi | 940 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
ChEMBL | Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.31 | pIC50 | 4900 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.31 | pIC50 | 4897.79 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
ChEMBL | Agonist activity at muscarinic M5 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5443-5447 [PMID:18829311] |
ChEMBL | Agonist activity at muscarinic M5 receptor | F | 4.3 | pEC50 | >50000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5439-5442 [PMID:18805692] |
ChEMBL | Partial agonist activity at human muscarinic M5 receptor expressed in CHO cells calcium response | F | 4.52 | pEC50 | >30000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
ChEMBL | Antagonist activity at rat muscarinic M5 receptor expressed in CHO cells assessed as inhibition of Ach-induced calcium response | F | 5.4 | pIC50 | 3970 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Binding affinity to human 5HT2C receptor agonist site by radioligand displacement assay | B | 7.07 | pKi | 85 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
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]