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Assay Detail

CHEMBL645565

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

Binding
In vitro binding affinity at human Alpha-1B adrenergic receptor.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous 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 as ligands for alpha(1)-adrenoceptor subtypes.
Romeo G, Materia L, Manetti F, Cagnotto A, Mennini T, Nicoletti F, Botta M, Russo F, Minneman KP.
J Med Chem (2003) 46 : 2877 -2894
PubMed 12825930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.95 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301707 1 8.74
CHEMBL57163 1 8.59
CHEMBL99761 1 8.54
CHEMBL99879 1 7.93
CHEMBL433203 1 7.86
CHEMBL317555 1 7.84
CHEMBL99142 1 7.68
CHEMBL316677 1 7.57
CHEMBL99979 1 7.56
CHEMBL433014 1 7.21
CHEMBL98807 1 6.79
CHEMBL329971 1 6.61
CHEMBL317556 1 5.69
CHEMBL100481 1 5.39
CHEMBL95605 1 5.11
CHEMBL100434 1 5.02
CHEMBL95986 1 4.00
CHEMBL99994 1 -
CHEMBL319345 1 -
CHEMBL98912 1 -
CHEMBL99363 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301707 Ki = 1.82 nM 8.74
CHEMBL57163 Ki = 2.57 nM 8.59
CHEMBL99761 Ki = 2.884 nM 8.54
CHEMBL99879 Ki = 11.75 nM 7.93
CHEMBL433203 Ki = 13.8 nM 7.86
CHEMBL317555 Ki = 14.45 nM 7.84
CHEMBL99142 Ki = 20.89 nM 7.68
CHEMBL316677 Ki = 26.92 nM 7.57
CHEMBL99979 Ki = 27.54 nM 7.56
CHEMBL433014 Ki = 61.66 nM 7.21
CHEMBL98807 Ki = 162.18 nM 6.79
CHEMBL329971 Ki = 245.47 nM 6.61
CHEMBL317556 Ki = 2041.74 nM 5.69
CHEMBL100481 Ki = 4073.8 nM 5.39
CHEMBL95605 Ki = 7762.47 nM 5.11
CHEMBL100434 Ki = 9549.93 nM 5.02
CHEMBL95986 Ki = 100000.0 nM 4.00
CHEMBL99994 Ki < 10000.0 nM -
CHEMBL319345 Ki = 55.0 nM -
CHEMBL98912 Ki < 10000.0 nM -
CHEMBL99363 Ki < 10000.0 nM -