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Assay Detail

CHEMBL645994

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

Binding
Binding affinity to rat alpha-1D adrenergic receptor expressed in LTK cells
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type LTK
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Alpha-1D adrenergic receptor (CHEMBL326)
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 8.66 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58956 1 9.68
CHEMBL62028 1 9.62
CHEMBL61598 1 9.39
CHEMBL445071 1 9.28
CHEMBL60471 1 9.24
CHEMBL61491 1 9.21
CHEMBL61483 1 9.18
CHEMBL293695 1 9.17
CHEMBL440865 1 9.16
CHEMBL60721 1 9.15
CHEMBL60510 1 9.14
CHEMBL369154 1 9.11
CHEMBL62033 1 9.11
CHEMBL431720 1 9.05
CHEMBL291839 1 9.04
CHEMBL2115086 1 9.04
CHEMBL292881 1 9.00
CHEMBL61225 1 8.95
CHEMBL62110 1 8.95
CHEMBL302203 1 8.94
CHEMBL304215 1 8.92
CHEMBL293236 1 8.86
CHEMBL291303 1 8.85
CHEMBL294027 1 8.84
CHEMBL291528 1 8.82
CHEMBL294098 1 8.78
CHEMBL432147 1 8.75
CHEMBL60722 1 8.70
CHEMBL299907 1 8.60
CHEMBL62109 1 8.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58956 Ki = 0.21 nM 9.68
CHEMBL62028 Ki = 0.24 nM 9.62
CHEMBL61598 Ki = 0.41 nM 9.39
CHEMBL445071 Ki = 0.52 nM 9.28
CHEMBL60471 Ki = 0.58 nM 9.24
CHEMBL61491 Ki = 0.62 nM 9.21
CHEMBL61483 Ki = 0.66 nM 9.18
CHEMBL293695 Ki = 0.68 nM 9.17
CHEMBL440865 Ki = 0.69 nM 9.16
CHEMBL60721 Ki = 0.71 nM 9.15
CHEMBL60510 Ki = 0.73 nM 9.14
CHEMBL62033 Ki = 0.77 nM 9.11
CHEMBL369154 Ki = 0.77 nM 9.11
CHEMBL431720 Ki = 0.89 nM 9.05
CHEMBL2115086 Ki = 0.92 nM 9.04
CHEMBL291839 Ki = 0.92 nM 9.04
CHEMBL292881 Ki = 1.01 nM 9.00
CHEMBL61225 Ki = 1.13 nM 8.95
CHEMBL62110 Ki = 1.13 nM 8.95
CHEMBL302203 Ki = 1.15 nM 8.94
CHEMBL304215 Ki = 1.2 nM 8.92
CHEMBL293236 Ki = 1.38 nM 8.86
CHEMBL291303 Ki = 1.4 nM 8.85
CHEMBL294027 Ki = 1.45 nM 8.84
CHEMBL291528 Ki = 1.5 nM 8.82
CHEMBL294098 Ki = 1.67 nM 8.78
CHEMBL432147 Ki = 1.78 nM 8.75
CHEMBL60722 Ki = 1.99 nM 8.70
CHEMBL299907 Ki = 2.5 nM 8.60
CHEMBL62109 Ki = 2.71 nM 8.57
CHEMBL291769 Ki = 2.86 nM 8.54
CHEMBL291588 Ki = 2.87 nM 8.54
CHEMBL58862 Ki = 3.71 nM 8.43
CHEMBL290387 Ki = 3.83 nM 8.42
CHEMBL58105 Ki = 4.4 nM 8.36
CHEMBL62206 Ki = 5.49 nM 8.26
CHEMBL445325 Ki = 7.79 nM 8.11
CHEMBL58612 Ki = 32.65 nM 7.49
CHEMBL291305 Ki = 58.4 nM 7.23
CHEMBL303988 Ki = 71.97 nM 7.14
CHEMBL59575 Ki = 83.4 nM 7.08
CHEMBL58585 Ki = 168.2 nM 6.77
CHEMBL302192 Ki = 189.0 nM 6.72