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Assay Detail

CHEMBL1947814

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Binding
Binding affinity to beta1 adrenoceptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-1 adrenergic receptor (CHEMBL213)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From libraries to candidate: the discovery of new ultra long-acting dibasic β₂-adrenoceptor agonists.
Alcaraz L, Bailey A, Cadogan E, Connolly S, Jewell R, Jordan S, Kindon N, Lister A, Lawson M, Mullen A, Dainty I, Nicholls D, Paine S, Pairaudeau G, Stocks MJ, Thorne P, Young A.
Bioorg Med Chem Lett (2012) 22 : 689 -695
PubMed 22079756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.40 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095777 INDACATEROL 4.0 1 6.50
CHEMBL1263 SALMETEROL 4.0 1 6.30
CHEMBL1256786 FORMOTEROL 4.0 1 -
CHEMBL82663 SIBENADET 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095777 INDACATEROL IC50 = 316.23 nM 6.50
CHEMBL1263 SALMETEROL IC50 = 501.19 nM 6.30
CHEMBL1256786 FORMOTEROL IC50 > 630.96 nM -
CHEMBL82663 SIBENADET IC50 > 10000.0 nM -