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Assay Detail

CHEMBL910638

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

Binding
Displacement of [3H]prazosin from cloned human adrenergic alpha 1A receptor expressed in CHO cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

WB4101-related compounds: new, subtype-selective alpha1-adrenoreceptor antagonists (or inverse agonists?).
Pallavicini M, Budriesi R, Fumagalli L, Ioan P, Chiarini A, Bolchi C, Ugenti MP, Colleoni S, Gobbi M, Valoti E.
J Med Chem (2006) 49 : 7140 -7149
PubMed 17125266 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.80 9.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215421 1 9.39
CHEMBL215151 1 8.92
CHEMBL217469 1 8.80
CHEMBL383938 1 8.55
CHEMBL439346 1 8.34
CHEMBL214694 1 8.25
CHEMBL214952 1 8.03
CHEMBL214986 1 7.95
CHEMBL217143 1 7.94
CHEMBL214552 1 7.79
CHEMBL218079 1 7.60
CHEMBL215188 1 7.47
CHEMBL385371 1 7.18
CHEMBL214762 1 7.06
CHEMBL215857 1 7.00
CHEMBL436955 1 6.99
CHEMBL214506 1 6.63
CHEMBL218732 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215421 Ki = 0.4074 nM 9.39
CHEMBL215151 Ki = 1.202 nM 8.92
CHEMBL217469 Ki = 1.585 nM 8.80
CHEMBL383938 Ki = 2.818 nM 8.55
CHEMBL439346 Ki = 4.571 nM 8.34
CHEMBL214694 Ki = 5.623 nM 8.25
CHEMBL214952 Ki = 9.333 nM 8.03
CHEMBL214986 Ki = 11.22 nM 7.95
CHEMBL217143 Ki = 11.48 nM 7.94
CHEMBL214552 Ki = 16.22 nM 7.79
CHEMBL218079 Ki = 25.12 nM 7.60
CHEMBL215188 Ki = 33.88 nM 7.47
CHEMBL385371 Ki = 66.07 nM 7.18
CHEMBL214762 Ki = 87.1 nM 7.06
CHEMBL215857 Ki = 100.0 nM 7.00
CHEMBL436955 Ki = 102.33 nM 6.99
CHEMBL214506 Ki = 234.42 nM 6.63
CHEMBL218732 Ki = 323.59 nM 6.49