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Assay Detail

CHEMBL646012

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

Binding
Binding affinity to alpha-1A adrenergic receptor in rat submaxillary gland
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Submaxillary gland
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL319) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity studies for a novel series of bicyclic substituted hexahydrobenz[e]isoindole alpha1A adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia.
Meyer MD, Altenbach RJ, Bai H, Basha FZ, Carroll WA, Kerwin JF, Lebold SA, Lee E, Pratt JK, Sippy KB, Tietje K, Wendt MD, Brune ME, Buckner SA, Hancock AA, Drizin I.
J Med Chem (2001) 44 : 1971 -1985
PubMed 11384242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 43 8.94 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL62028 — — 1 10.40
CHEMBL293695 — — 1 10.40
CHEMBL62033 — — 1 10.05
CHEMBL58956 — — 1 10.05
CHEMBL431720 — — 1 10.05
CHEMBL291303 — — 1 9.62
CHEMBL58862 — — 1 9.60
CHEMBL445325 — — 1 9.57
CHEMBL369154 — — 1 9.57
CHEMBL61483 — — 1 9.48
CHEMBL291528 — — 1 9.39
CHEMBL61598 — — 1 9.37
CHEMBL445071 — — 1 9.32
CHEMBL60471 — — 1 9.24
CHEMBL61491 — — 1 9.17
CHEMBL290387 — — 1 9.16
CHEMBL440865 — — 1 9.15
CHEMBL60721 — — 1 9.07
CHEMBL302203 — — 1 9.07
CHEMBL304215 — — 1 9.04
CHEMBL292881 — — 1 8.99
CHEMBL61225 — — 1 8.99
CHEMBL294027 — — 1 8.96
CHEMBL62110 — — 1 8.94
CHEMBL60722 — — 1 8.92
CHEMBL294098 — — 1 8.92
CHEMBL60510 — — 1 8.86
CHEMBL2115086 — — 1 8.86
CHEMBL291839 — — 1 8.86
CHEMBL432147 — — 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL62028 — Ki = 0.04 nM 10.40
CHEMBL293695 — Ki = 0.04 nM 10.40
CHEMBL58956 — Ki = 0.09 nM 10.05
CHEMBL431720 — Ki = 0.09 nM 10.05
CHEMBL62033 — Ki = 0.09 nM 10.05
CHEMBL291303 — Ki = 0.24 nM 9.62
CHEMBL58862 — Ki = 0.25 nM 9.60
CHEMBL445325 — Ki = 0.27 nM 9.57
CHEMBL369154 — Ki = 0.27 nM 9.57
CHEMBL61483 — Ki = 0.33 nM 9.48
CHEMBL291528 — Ki = 0.41 nM 9.39
CHEMBL61598 — Ki = 0.43 nM 9.37
CHEMBL445071 — Ki = 0.48 nM 9.32
CHEMBL60471 — Ki = 0.57 nM 9.24
CHEMBL61491 — Ki = 0.67 nM 9.17
CHEMBL290387 — Ki = 0.69 nM 9.16
CHEMBL440865 — Ki = 0.71 nM 9.15
CHEMBL60721 — Ki = 0.85 nM 9.07
CHEMBL302203 — Ki = 0.85 nM 9.07
CHEMBL304215 — Ki = 0.91 nM 9.04
CHEMBL61225 — Ki = 1.02 nM 8.99
CHEMBL292881 — Ki = 1.03 nM 8.99
CHEMBL294027 — Ki = 1.09 nM 8.96
CHEMBL62110 — Ki = 1.15 nM 8.94
CHEMBL60722 — Ki = 1.19 nM 8.92
CHEMBL294098 — Ki = 1.2 nM 8.92
CHEMBL60510 — Ki = 1.38 nM 8.86
CHEMBL2115086 — Ki = 1.39 nM 8.86
CHEMBL291839 — Ki = 1.39 nM 8.86
CHEMBL432147 — Ki = 1.41 nM 8.85
CHEMBL293236 — Ki = 1.48 nM 8.83
CHEMBL62109 — Ki = 1.89 nM 8.72
CHEMBL291769 — Ki = 2.73 nM 8.56
CHEMBL299907 — Ki = 3.58 nM 8.45
CHEMBL58612 — Ki = 3.75 nM 8.43
CHEMBL291588 — Ki = 6.8 nM 8.17
CHEMBL291305 — Ki = 7.82 nM 8.11
CHEMBL58105 — Ki = 7.73 nM 8.11
CHEMBL62206 — Ki = 9.22 nM 8.04
CHEMBL303988 — Ki = 12.9 nM 7.89
CHEMBL302192 — Ki = 62.22 nM 7.21
CHEMBL59575 — Ki = 80.7 nM 7.09
CHEMBL58585 — Ki = 122.6 nM 6.91