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 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]
