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Assay Detail

CHEMBL903398

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

Binding
Displacement of [3H]MK-912 from adrenergic alpha2A receptor in HT29 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HT-29
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Alpha-2A adrenergic receptor (CHEMBL1867)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel 4-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)methylbenzofuran derivatives as selective alpha(2C)-adrenergic receptor antagonists.
Hagihara K, Kashima H, Iida K, Enokizono J, Uchida S, Nonaka H, Kurokawa M, Shimada J.
Bioorg Med Chem Lett (2007) 17 : 1616 -1621
PubMed 17257841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.77 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL537669 YOHIMBINE HYDROCHLORIDE 3.0 1 8.74
CHEMBL10316 IDAZOXAN 3.0 1 8.10
CHEMBL394218 1 7.38
CHEMBL246229 1 6.87
CHEMBL247664 1 6.85
CHEMBL247665 1 6.73
CHEMBL392991 1 6.69
CHEMBL392771 1 6.67
CHEMBL246852 1 6.52
CHEMBL246228 1 6.40
CHEMBL428407 1 6.34
CHEMBL393597 1 6.07
CHEMBL392992 1 5.76
CHEMBL246639 1 5.59
CHEMBL246434 1 -
CHEMBL246435 1 -
CHEMBL438123 1 -
CHEMBL247467 1 -
CHEMBL247466 1 -
CHEMBL247057 1 -
CHEMBL247056 1 -
CHEMBL393783 1 -
CHEMBL246851 1 -
CHEMBL246640 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL537669 YOHIMBINE HYDROCHLORIDE Ki = 1.8 nM 8.74
CHEMBL10316 IDAZOXAN Ki = 8.0 nM 8.10
CHEMBL394218 Ki = 42.0 nM 7.38
CHEMBL246229 Ki = 135.0 nM 6.87
CHEMBL247664 Ki = 141.0 nM 6.85
CHEMBL247665 Ki = 186.0 nM 6.73
CHEMBL392991 Ki = 204.0 nM 6.69
CHEMBL392771 Ki = 216.0 nM 6.67
CHEMBL246852 Ki = 304.0 nM 6.52
CHEMBL246228 Ki = 400.0 nM 6.40
CHEMBL428407 Ki = 454.0 nM 6.34
CHEMBL393597 Ki = 857.0 nM 6.07
CHEMBL392992 Ki = 1742.0 nM 5.76
CHEMBL246639 Ki = 2552.0 nM 5.59
CHEMBL246434 Ki - -
CHEMBL246435 Ki - -
CHEMBL438123 Ki - -
CHEMBL247467 Ki - -
CHEMBL247466 Ki - -
CHEMBL247057 Ki - -
CHEMBL247056 Ki - -
CHEMBL393783 Ki - -
CHEMBL246851 Ki - -
CHEMBL246640 Ki - -