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Assay Detail

CHEMBL654956

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Binding
Activity at beta-1 adrenergic receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Beta-1 adrenergic receptor (CHEMBL5471)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Computer-aided mapping of the beta-adrenoceptor. 1. Explanation for effect of para substitution on blocking activity at the beta-1-adrenoceptor.
Ball JB, Nero TL, Iakovidis D, Tung L, Jackman G, Louis WJ.
J Med Chem (1992) 35 : 4676 -4682
PubMed 1361581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 7.17 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11171 1 8.90
CHEMBL43405 1 8.20
CHEMBL269219 1 7.60
CHEMBL143467 1 7.20
CHEMBL768 ESMOLOL 4.0 1 7.00
CHEMBL24 ATENOLOL 4.0 1 6.80
CHEMBL31608 1 6.50
CHEMBL31036 1 6.30
CHEMBL6995 PRACTOLOL 4.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11171 Kd = 1.259 nM 8.90
CHEMBL43405 Kd = 6.31 nM 8.20
CHEMBL269219 Kd = 25.12 nM 7.60
CHEMBL143467 Kd = 63.1 nM 7.20
CHEMBL768 ESMOLOL Kd = 100.0 nM 7.00
CHEMBL24 ATENOLOL Kd = 158.49 nM 6.80
CHEMBL31608 Kd = 316.23 nM 6.50
CHEMBL31036 Kd = 501.19 nM 6.30
CHEMBL6995 PRACTOLOL Kd = 1000.0 nM 6.00