TBPB [Ligand Id: 3258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL522460
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Rat [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Rat [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
  • M3 receptor/Muscarinic acetylcholine receptor M3 in Rat [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
  • M4 receptor/Muscarinic acetylcholine receptor M4 in Rat [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
  • M5 receptor/Muscarinic acetylcholine receptor M5 in Rat [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]