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Assay Detail

CHEMBL2091585

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human beta1-adrenoceptor by radioligand binding assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.
Beattie D, Beer D, Bradley ME, Bruce I, Charlton SJ, Cuenoud BM, Fairhurst RA, Farr D, Fozard JR, Janus D, Rosethorne EM, Sandham DA, Sykes DA, Trifilieff A, Turner KL, Wissler E.
Bioorg Med Chem Lett (2012) 22 : 6280 -6285
PubMed 22932315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.71 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2088201 1 8.72
CHEMBL2088202 1 6.88
CHEMBL1346 DARIFENACIN 4.0 1 6.75
CHEMBL2088197 1 6.74
CHEMBL2088196 1 6.64
CHEMBL2088199 1 6.59
CHEMBL2088200 1 6.38
CHEMBL2088198 1 6.32
CHEMBL82663 SIBENADET 2.0 1 5.41
CHEMBL2088195 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2088201 Ki = 1.9 nM 8.72
CHEMBL2088202 Ki = 133.0 nM 6.88
CHEMBL1346 DARIFENACIN Ki = 180.0 nM 6.75
CHEMBL2088197 Ki = 183.0 nM 6.74
CHEMBL2088196 Ki = 227.0 nM 6.64
CHEMBL2088199 Ki = 259.0 nM 6.59
CHEMBL2088200 Ki = 421.0 nM 6.38
CHEMBL2088198 Ki = 478.0 nM 6.32
CHEMBL82663 SIBENADET Ki = 3922.0 nM 5.41
CHEMBL2088195 Ki > 10000.0 nM -