Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL646002

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

Binding
In vitro binding affinity using [3H]prazosin as radioligand against alpha-1D adrenergic receptor expressed in LTK cell
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1D adrenergic receptor (CHEMBL326)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Condon S, Elmore SW, Kerwin JF, Sippy KB, Tietje K, Wendt MD, Hancock AA, Brune ME, Buckner SA, Drizin I.
J Med Chem (2000) 43 : 1586 -1603
PubMed 10780916 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 8.72 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL291073 1 9.57
CHEMBL287965 1 9.55
CHEMBL41444 1 9.51
CHEMBL40754 1 9.43
CHEMBL289361 2 9.43
CHEMBL290388 1 9.29
CHEMBL40650 1 9.29
CHEMBL41155 1 9.23
CHEMBL290519 1 9.20
CHEMBL417890 1 9.17
CHEMBL291262 1 9.16
CHEMBL40780 1 9.13
CHEMBL288809 1 9.13
CHEMBL39037 1 9.06
CHEMBL2112073 2 9.03
CHEMBL40310 1 8.98
CHEMBL41344 1 8.97
CHEMBL41234 1 8.96
CHEMBL441032 1 8.96
CHEMBL291154 1 8.88
CHEMBL40819 1 8.88
CHEMBL287928 1 8.85
CHEMBL288530 1 8.69
CHEMBL288678 1 8.68
CHEMBL289627 1 8.68
CHEMBL297218 1 8.64
CHEMBL43573 1 8.55
CHEMBL290243 1 8.48
CHEMBL40896 1 8.43
CHEMBL289437 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL291073 Ki = 0.27 nM 9.57
CHEMBL287965 Ki = 0.28 nM 9.55
CHEMBL41444 Ki = 0.31 nM 9.51
CHEMBL40754 Ki = 0.37 nM 9.43
CHEMBL289361 Ki = 0.37 nM 9.43
CHEMBL290388 Ki = 0.51 nM 9.29
CHEMBL40650 Ki = 0.51 nM 9.29
CHEMBL41155 Ki = 0.59 nM 9.23
CHEMBL289361 Ki = 0.63 nM 9.20
CHEMBL290519 Ki = 0.63 nM 9.20
CHEMBL417890 Ki = 0.68 nM 9.17
CHEMBL291262 Ki = 0.69 nM 9.16
CHEMBL288809 Ki = 0.74 nM 9.13
CHEMBL40780 Ki = 0.74 nM 9.13
CHEMBL39037 Ki = 0.88 nM 9.06
CHEMBL2112073 Ki = 0.94 nM 9.03
CHEMBL40310 Ki = 1.04 nM 8.98
CHEMBL41344 Ki = 1.07 nM 8.97
CHEMBL441032 Ki = 1.1 nM 8.96
CHEMBL41234 Ki = 1.1 nM 8.96
CHEMBL40819 Ki = 1.31 nM 8.88
CHEMBL291154 Ki = 1.32 nM 8.88
CHEMBL287928 Ki = 1.41 nM 8.85
CHEMBL288530 Ki = 2.06 nM 8.69
CHEMBL289627 Ki = 2.08 nM 8.68
CHEMBL288678 Ki = 2.08 nM 8.68
CHEMBL297218 Ki = 2.31 nM 8.64
CHEMBL43573 Ki = 2.84 nM 8.55
CHEMBL290243 Ki = 3.28 nM 8.48
CHEMBL40896 Ki = 3.74 nM 8.43
CHEMBL289437 Ki = 4.16 nM 8.38
CHEMBL289758 Ki = 4.77 nM 8.32
CHEMBL43921 Ki = 5.76 nM 8.24
CHEMBL2112073 Ki = 6.28 nM 8.20
CHEMBL289166 Ki = 6.6 nM 8.18
CHEMBL43234 Ki = 6.84 nM 8.16
CHEMBL40564 Ki = 7.7 nM 8.11
CHEMBL434591 Ki = 8.67 nM 8.06
CHEMBL43909 Ki = 19.8 nM 7.70
CHEMBL41396 Ki = 25.0 nM 7.60
CHEMBL41332 Ki = 47.0 nM 7.33
CHEMBL296711 Ki = 160.0 nM 6.80