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Assay Detail

CHEMBL912602

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

Binding
Displacement of [125I]BE2254 from human cloned adrenergic alpha 1B receptor expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Romeo G, Materia L, Marucci G, Modica M, Pittalà V, Salerno L, Siracusa MA, Buccioni M, Angeli P, Minneman KP.
Bioorg Med Chem Lett (2006) 16 : 6200 -6203
PubMed 17027264 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.40 8.74
Log Ki 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301707 1 8.74
CHEMBL220515 1 8.35
CHEMBL220781 1 8.05
CHEMBL386005 1 7.97
CHEMBL222896 1 7.76
CHEMBL220221 1 7.76
CHEMBL99142 1 7.68
CHEMBL220717 1 7.08
CHEMBL223289 1 7.04
CHEMBL219719 1 6.22
CHEMBL219718 1 4.72
CHEMBL223842 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301707 Ki = 1.82 nM 8.74
CHEMBL220515 Ki = 4.467 nM 8.35
CHEMBL220781 Ki = 8.913 nM 8.05
CHEMBL386005 Ki = 10.72 nM 7.97
CHEMBL222896 Ki = 17.38 nM 7.76
CHEMBL220221 Ki = 17.38 nM 7.76
CHEMBL99142 Ki = 20.89 nM 7.68
CHEMBL220717 Ki = 83.18 nM 7.08
CHEMBL223289 Ki = 91.2 nM 7.04
CHEMBL219719 Ki = 602.56 nM 6.22
CHEMBL219718 Ki = 19054.61 nM 4.72
CHEMBL223842 Log Ki - -