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Assay Detail

CHEMBL645797

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

Binding
Displacement of prazosin from Alpha-1 adrenergic receptors of human cerebral cortex homogenate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and evaluation of 2-(arylamino)imidazoles as alpha 2-adrenergic agonists.
Munk SA, Harcourt DA, Arasasingham PN, Burke JA, Kharlamb AB, Manlapaz CA, Padillo EU, Roberts D, Runde E, Williams L, Wheeler LA, Garst ME.
J Med Chem (1997) 40 : 18 -23
PubMed 9016324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.21 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49137 1 5.85
CHEMBL844 BRIMONIDINE 4.0 1 5.75
CHEMBL308570 1 5.68
CHEMBL75257 1 5.38
CHEMBL1022 1 5.22
CHEMBL308863 1 5.18
CHEMBL77913 1 5.08
CHEMBL76457 1 4.96
CHEMBL432155 1 4.80
CHEMBL78190 1 4.80
CHEMBL74544 1 4.62
CHEMBL75491 1 -
CHEMBL1019 1 -
CHEMBL74449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49137 Ki = 1400.0 nM 5.85
CHEMBL844 BRIMONIDINE Ki = 1800.0 nM 5.75
CHEMBL308570 Ki = 2100.0 nM 5.68
CHEMBL75257 Ki = 4200.0 nM 5.38
CHEMBL1022 Ki = 6000.0 nM 5.22
CHEMBL308863 Ki = 6600.0 nM 5.18
CHEMBL77913 Ki = 8400.0 nM 5.08
CHEMBL76457 Ki = 11000.0 nM 4.96
CHEMBL432155 Ki = 16000.0 nM 4.80
CHEMBL78190 Ki = 16000.0 nM 4.80
CHEMBL74544 Ki = 24000.0 nM 4.62
CHEMBL75491 Ki > 28000.0 nM -
CHEMBL1019 Ki > 100000.0 nM -
CHEMBL74449 Ki > 100000.0 nM -