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

CHEMBL644963

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
26
Total Activities
26
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 26 6.94 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64420 1 8.07
CHEMBL60900 1 8.02
CHEMBL304894 1 7.96
CHEMBL59737 1 7.94
CHEMBL61671 1 7.89
CHEMBL302436 1 7.60
CHEMBL60265 1 7.58
CHEMBL59501 1 7.39
CHEMBL60783 1 7.22
CHEMBL294204 1 7.18
CHEMBL60840 1 7.01
CHEMBL64134 1 6.86
CHEMBL292253 1 6.84
CHEMBL62290 1 6.81
CHEMBL303556 1 6.78
CHEMBL64345 1 6.64
CHEMBL300316 1 6.57
CHEMBL61665 1 6.57
CHEMBL294538 1 6.54
CHEMBL305585 1 6.48
CHEMBL435182 1 6.46
CHEMBL59500 1 6.37
CHEMBL60361 1 6.34
CHEMBL64283 1 6.17
CHEMBL64238 1 5.98
CHEMBL64508 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64420 Ki = 8.5 nM 8.07
CHEMBL60900 Ki = 9.5 nM 8.02
CHEMBL304894 Ki = 11.0 nM 7.96
CHEMBL59737 Ki = 11.5 nM 7.94
CHEMBL61671 Ki = 13.0 nM 7.89
CHEMBL302436 Ki = 25.0 nM 7.60
CHEMBL60265 Ki = 26.0 nM 7.58
CHEMBL59501 Ki = 41.0 nM 7.39
CHEMBL60783 Ki = 60.0 nM 7.22
CHEMBL294204 Ki = 66.0 nM 7.18
CHEMBL60840 Ki = 97.5 nM 7.01
CHEMBL64134 Ki = 138.5 nM 6.86
CHEMBL292253 Ki = 143.0 nM 6.84
CHEMBL62290 Ki = 154.0 nM 6.81
CHEMBL303556 Ki = 165.0 nM 6.78
CHEMBL64345 Ki = 229.0 nM 6.64
CHEMBL300316 Ki = 268.0 nM 6.57
CHEMBL61665 Ki = 268.0 nM 6.57
CHEMBL294538 Ki = 292.0 nM 6.54
CHEMBL305585 Ki = 334.0 nM 6.48
CHEMBL435182 Ki = 350.0 nM 6.46
CHEMBL59500 Ki = 431.0 nM 6.37
CHEMBL60361 Ki = 458.0 nM 6.34
CHEMBL64283 Ki = 675.0 nM 6.17
CHEMBL64238 Ki = 1057.0 nM 5.98
CHEMBL64508 Ki = 5291.0 nM 5.28