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Assay Detail

CHEMBL644960

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

Binding
In vitro binding affinity towards Alpha-1 adrenergic receptor by the displacement of [3H]prazosin radioligand in rat cortical homogenates
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.
Mewshaw RE, Webb MB, Marquis KL, McGaughey GB, Shi X, Wasik T, Scerni R, Brennan JA, Andree TH.
J Med Chem (1999) 42 : 2007 -2020
PubMed 10354409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.75 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL60548 1 8.30
CHEMBL64466 1 7.85
CHEMBL60185 1 7.62
CHEMBL64574 1 7.50
CHEMBL418510 1 7.41
CHEMBL63491 1 7.28
CHEMBL64524 1 7.07
CHEMBL291459 1 6.89
CHEMBL302000 1 6.87
CHEMBL64553 1 6.67
CHEMBL64798 1 6.66
CHEMBL300571 1 6.59
CHEMBL59750 1 6.42
CHEMBL59752 1 5.84
CHEMBL418681 1 5.54
CHEMBL434407 1 5.32
CHEMBL416856 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL60548 Ki = 5.0 nM 8.30
CHEMBL64466 Ki = 14.0 nM 7.85
CHEMBL60185 Ki = 24.0 nM 7.62
CHEMBL64574 Ki = 32.0 nM 7.50
CHEMBL418510 Ki = 39.0 nM 7.41
CHEMBL63491 Ki = 52.0 nM 7.28
CHEMBL64524 Ki = 85.0 nM 7.07
CHEMBL291459 Ki = 128.0 nM 6.89
CHEMBL302000 Ki = 134.0 nM 6.87
CHEMBL64553 Ki = 212.0 nM 6.67
CHEMBL64798 Ki = 220.0 nM 6.66
CHEMBL300571 Ki = 254.0 nM 6.59
CHEMBL59750 Ki = 380.0 nM 6.42
CHEMBL59752 Ki = 1448.0 nM 5.84
CHEMBL418681 Ki = 2899.0 nM 5.54
CHEMBL434407 Ki = 4829.0 nM 5.32
CHEMBL416856 Ki = 11081.0 nM 4.96