LK 204-545 [Ligand Id: 544] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL207802 (LK-204545) |
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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]; FASEB J (2017) 31: 3150-3166 [PMID:28400472] |
| 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 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]
