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Assay Detail

CHEMBL645555

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

Binding
Displacement of [3H]prazosin from rat cortex Alpha-1 adrenergic receptor
13
Total Activities
13
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

Design, synthesis, and structure-activity relationships of a new series of alpha-adrenergic agonists: spiro[(1,3-diazacyclopent-1-ene)-5,2'-(1',2',3',4'- tetrahydronaphthalene)].
Cordi AA, Lacoste JM, Descombes JJ, Courchay C, Vanhoutte PM, Laubie M, Verbeuren TJ.
J Med Chem (1995) 38 : 4056 -4069
PubMed 7562941 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 5.43 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131539 1 6.22
CHEMBL130784 1 6.22
CHEMBL338683 1 6.16
CHEMBL133231 1 6.10
CHEMBL98471 1 6.00
CHEMBL336331 1 5.70
CHEMBL131220 1 5.60
CHEMBL336332 1 5.47
CHEMBL130853 1 4.84
CHEMBL133579 1 4.80
CHEMBL131417 1 4.80
CHEMBL336970 1 4.53
CHEMBL101340 1 4.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131539 Ki = 600.0 nM 6.22
CHEMBL130784 Ki = 600.0 nM 6.22
CHEMBL338683 Ki = 700.0 nM 6.16
CHEMBL133231 Ki = 800.0 nM 6.10
CHEMBL98471 Ki = 1000.0 nM 6.00
CHEMBL336331 Ki = 2000.0 nM 5.70
CHEMBL131220 Ki = 2500.0 nM 5.60
CHEMBL336332 Ki = 3400.0 nM 5.47
CHEMBL130853 Ki = 14400.0 nM 4.84
CHEMBL133579 Ki = 16000.0 nM 4.80
CHEMBL131417 Ki = 16000.0 nM 4.80
CHEMBL336970 Ki = 29400.0 nM 4.53
CHEMBL101340 Ki = 65800.0 nM 4.18