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 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]