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Assay Detail

CHEMBL645393

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

Binding
Binding affinity towards alpha-1 adrenergic receptor in rat cortex membrane using [3H]-prazosin radioligand
ChEMBL ↗
60
Total Activities
60
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

Synthesis, biological evaluation, and pharmacophore generation of new pyridazinone derivatives with affinity toward alpha(1)- and alpha(2)-adrenoceptors.
Barbaro R, Betti L, Botta M, Corelli F, Giannaccini G, Maccari L, Manetti F, Strappaghetti G, Corsano S.
J Med Chem (2001) 44 : 2118 -2132
PubMed 11405649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 60 7.91 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.62
CHEMBL66450 — — 1 9.22
CHEMBL68052 — — 1 9.10
CHEMBL49152 — — 1 8.85
CHEMBL66172 — — 1 8.82
CHEMBL46172 — — 1 8.72
CHEMBL67201 — — 1 8.72
CHEMBL302554 — — 1 8.64
CHEMBL67132 — — 1 8.57
CHEMBL66272 — — 1 8.46
CHEMBL302832 — — 1 8.46
CHEMBL65963 — — 1 8.44
CHEMBL67379 — — 1 8.41
CHEMBL304783 — — 1 8.41
CHEMBL302268 — — 1 8.39
CHEMBL303347 — — 1 8.38
CHEMBL66747 — — 1 8.37
CHEMBL303894 — — 1 8.35
CHEMBL302857 — — 1 8.25
CHEMBL304325 — — 1 8.25
CHEMBL68447 — — 1 8.24
CHEMBL66965 — — 1 8.23
CHEMBL67681 — — 1 8.17
CHEMBL67773 — — 1 8.15
CHEMBL67081 — — 1 8.15
CHEMBL67882 — — 1 8.14
CHEMBL417745 — — 1 8.10
CHEMBL441444 — — 1 8.10
CHEMBL306440 — — 1 8.08
CHEMBL303895 — — 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.24 nM 9.62
CHEMBL66450 — Ki = 0.6 nM 9.22
CHEMBL68052 — Ki = 0.8 nM 9.10
CHEMBL49152 — Ki = 1.4 nM 8.85
CHEMBL66172 — Ki = 1.5 nM 8.82
CHEMBL46172 — Ki = 1.9 nM 8.72
CHEMBL67201 — Ki = 1.9 nM 8.72
CHEMBL302554 — Ki = 2.3 nM 8.64
CHEMBL67132 — Ki = 2.7 nM 8.57
CHEMBL66272 — Ki = 3.5 nM 8.46
CHEMBL302832 — Ki = 3.5 nM 8.46
CHEMBL65963 — Ki = 3.6 nM 8.44
CHEMBL67379 — Ki = 3.9 nM 8.41
CHEMBL304783 — Ki = 3.9 nM 8.41
CHEMBL302268 — Ki = 4.1 nM 8.39
CHEMBL303347 — Ki = 4.2 nM 8.38
CHEMBL66747 — Ki = 4.3 nM 8.37
CHEMBL303894 — Ki = 4.5 nM 8.35
CHEMBL302857 — Ki = 5.6 nM 8.25
CHEMBL304325 — Ki = 5.6 nM 8.25
CHEMBL68447 — Ki = 5.7 nM 8.24
CHEMBL66965 — Ki = 5.9 nM 8.23
CHEMBL67681 — Ki = 6.8 nM 8.17
CHEMBL67773 — Ki = 7.0 nM 8.15
CHEMBL67081 — Ki = 7.0 nM 8.15
CHEMBL67882 — Ki = 7.3 nM 8.14
CHEMBL441444 — Ki = 7.9 nM 8.10
CHEMBL417745 — Ki = 7.9 nM 8.10
CHEMBL306440 — Ki = 8.4 nM 8.08
CHEMBL303895 — Ki = 10.0 nM 8.00
CHEMBL67114 — Ki = 11.5 nM 7.94
CHEMBL66748 — Ki = 12.9 nM 7.89
CHEMBL63876 — Ki = 12.8 nM 7.89
CHEMBL417565 — Ki = 13.3 nM 7.88
CHEMBL67639 — Ki = 14.5 nM 7.84
CHEMBL302051 — Ki = 15.0 nM 7.82
CHEMBL444582 — Ki = 15.6 nM 7.81
CHEMBL303130 — Ki = 16.0 nM 7.80
CHEMBL70173 — Ki = 17.8 nM 7.75
CHEMBL63781 — Ki = 18.0 nM 7.75
CHEMBL305173 — Ki = 19.0 nM 7.72
CHEMBL67218 — Ki = 20.4 nM 7.69
CHEMBL301726 — Ki = 24.6 nM 7.61
CHEMBL431721 — Ki = 27.8 nM 7.56
CHEMBL67478 — Ki = 33.0 nM 7.48
CHEMBL65887 — Ki = 34.0 nM 7.47
CHEMBL67162 — Ki = 33.5 nM 7.47
CHEMBL66118 — Ki = 38.0 nM 7.42
CHEMBL303219 — Ki = 42.7 nM 7.37
CHEMBL67856 — Ki = 43.7 nM 7.36