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Assay Detail

CHEMBL647963

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

Binding
Binding affinity against human Alpha-2A adrenergic receptor expressed stably in CHO cells using [3H]rauwolscine as radioligand
11
Total Activities
11
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-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Yohimbine dimers exhibiting binding selectivities for human alpha2a- versus alpha2b-adrenergic receptors.
Zheng W, Lei L, Lalchandani S, Sun G, Feller DR, Miller DD.
Bioorg Med Chem Lett (2000) 10 : 627 -630
PubMed 10762040 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.65 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL554019 1 9.41
CHEMBL15245 YOHIMBINE 3.0 1 9.38
CHEMBL538808 1 9.12
CHEMBL543232 1 9.06
CHEMBL551711 1 8.93
CHEMBL539606 1 8.90
CHEMBL542527 1 8.87
CHEMBL555190 1 8.76
CHEMBL539824 1 7.82
CHEMBL542520 1 7.58
CHEMBL540594 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL554019 Ki = 0.39 nM 9.41
CHEMBL15245 YOHIMBINE Ki = 0.42 nM 9.38
CHEMBL538808 Ki = 0.76 nM 9.12
CHEMBL543232 Ki = 0.87 nM 9.06
CHEMBL551711 Ki = 1.18 nM 8.93
CHEMBL539606 Ki = 1.25 nM 8.90
CHEMBL542527 Ki = 1.35 nM 8.87
CHEMBL555190 Ki = 1.73 nM 8.76
CHEMBL539824 Ki = 15.3 nM 7.82
CHEMBL542520 Ki = 26.4 nM 7.58
CHEMBL540594 Ki = 52.0 nM 7.28