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Assay Detail

CHEMBL648055

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

Binding
Evaluated for its ability to displace [3H]clonidine from alpha-2 adrenergic receptor of calf cerebral cortex
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-2A adrenergic receptor (CHEMBL4744)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.
Huff JR, Anderson PS, Baldwin JJ, Clineschmidt BV, Guare JP, Lotti VJ, Pettibone DJ, Randall WC, Vacca JP.
J Med Chem (1985) 28 : 1756 -1759
PubMed 2999400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.07 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48603 1 9.11
CHEMBL48558 1 8.87
CHEMBL15245 YOHIMBINE 3.0 1 7.31
CHEMBL299595 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48603 Ki = 0.77 nM 9.11
CHEMBL48558 Ki = 1.36 nM 8.87
CHEMBL15245 YOHIMBINE Ki = 49.0 nM 7.31
CHEMBL299595 Ki = 100.0 nM 7.00