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Assay Detail

CHEMBL1804370

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Functional
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type H292
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design driven HtL: The discovery and synthesis of new high efficacy β₂-agonists.
Stocks MJ, Alcaraz L, Bailey A, Bonnert R, Cadogan E, Christie J, Connolly S, Cook A, Fisher A, Flaherty A, Hill S, Humphries A, Ingall A, Jordan S, Lawson M, Mullen A, Nicholls D, Paine S, Pairaudeau G, St-Gallay S, Young A.
Bioorg Med Chem Lett (2011) 21 : 4027 -4031
PubMed 21652207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.26 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1800472 1 9.70
CHEMBL1256786 FORMOTEROL 4.0 1 9.30
CHEMBL323776 1 9.30
CHEMBL1800660 1 9.10
CHEMBL1263 SALMETEROL 4.0 1 9.10
CHEMBL1800656 1 9.00
CHEMBL1800659 1 8.80
CHEMBL111775 1 8.80
CHEMBL1800658 1 8.10
CHEMBL1800474 1 8.10
CHEMBL1800657 1 8.10
CHEMBL434 ISOPROTERENOL 4.0 1 7.40
CHEMBL1800475 1 6.90
CHEMBL714 ALBUTEROL 4.0 1 6.70
CHEMBL1760 TERBUTALINE 4.0 1 5.50
CHEMBL111732 1 -
CHEMBL1800473 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1800472 EC50 = 0.1995 nM 9.70
CHEMBL1256786 FORMOTEROL EC50 = 0.5012 nM 9.30
CHEMBL323776 EC50 = 0.5012 nM 9.30
CHEMBL1800660 EC50 = 0.7943 nM 9.10
CHEMBL1263 SALMETEROL EC50 = 0.7943 nM 9.10
CHEMBL1800656 EC50 = 1.0 nM 9.00
CHEMBL1800659 EC50 = 1.585 nM 8.80
CHEMBL111775 EC50 = 1.585 nM 8.80
CHEMBL1800658 EC50 = 7.943 nM 8.10
CHEMBL1800474 EC50 = 7.943 nM 8.10
CHEMBL1800657 EC50 = 7.943 nM 8.10
CHEMBL434 ISOPROTERENOL EC50 = 39.81 nM 7.40
CHEMBL1800475 EC50 = 125.89 nM 6.90
CHEMBL714 ALBUTEROL EC50 = 199.53 nM 6.70
CHEMBL1760 TERBUTALINE EC50 = 3162.28 nM 5.50
CHEMBL111732 EC50 > 1000.0 nM -
CHEMBL1800473 EC50 > 1000.0 nM -