LK 204-545 [Ligand Id: 544] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL207802 (LK-204545)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 8.04 pKd 9.12 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 8.77 pKd 1.7 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
GtoPdb - - 8.5 pKi - - - Eur. J. Pharmacol. (1999) 367: 431-5 [PMID:10079020]
ChEMBL Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 8.64 pEC50 2.29 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells F 4.1 pKi 79432.82 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells F 7 pKi 100 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells F 7.1 pKi 79.43 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells F 7.2 pKi 63.1 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells F 8.1 pKi 7.94 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 5.29 pKd 5128.61 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 5.54 pKd 2884.03 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
GtoPdb - - 5.2 pKi - - - Eur. J. Pharmacol. (1999) 367: 431-5 [PMID:10079020]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 5 pEC50 10000 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 5 pKd >10000 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 5 pEC50 10000 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]