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Assay Detail

CHEMBL652803

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

Binding
In vitro binding affinity towards alpha-1A adrenergic receptor of bovine clone in radioligand binding assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1A adrenergic receptor (CHEMBL4892)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis and structure-activity studies on N-[5-(1H-imidazol-4-yl)-5,6,7,8-tetrahydro-1-naphthalenyl]methanesulfonamide, an imidazole-containing alpha(1A)-adrenoceptor agonist.
Altenbach RJ, Khilevich A, Kolasa T, Rohde JJ, Bhatia PA, Patel MV, Searle XB, Yang F, Bunnelle WH, Tietje K, Bayburt EK, Carroll WA, Meyer MD, Henry R, Buckner SA, Kuk J, Daza AV, Milicic IV, Cain JC, Kang CH, Ireland LM, Carr TL, Miller TR, Hancock AA, Nakane M, Esbenshade TA, Brune ME, O'Neill AB, Gauvin DM, Katwala SP, Holladay MW, Brioni JD, Sullivan JP.
J Med Chem (2004) 47 : 3220 -3235
PubMed 15163201 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.42 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317912 1 6.94
CHEMBL323402 1 6.86
CHEMBL109827 1 6.83
CHEMBL112814 1 6.16
CHEMBL326862 1 6.01
CHEMBL327116 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317912 Ki = 114.82 nM 6.94
CHEMBL323402 Ki = 138.04 nM 6.86
CHEMBL109827 Ki = 147.91 nM 6.83
CHEMBL112814 Ki = 691.83 nM 6.16
CHEMBL326862 Ki = 977.24 nM 6.01
CHEMBL327116 Ki = 2041.74 nM 5.69