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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 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]