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Assay Detail

CHEMBL894443

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

Binding
Displacement of [125I]HEAT from human recombinant adrenergic alpha-1A receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL229)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR.
J Med Chem (2007) 50 : 3883 -3890
PubMed 17668922 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.36 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185271 SNAP-7941 1 7.40
CHEMBL363548 CHLOROHALOPERIDOL 1 6.82
CHEMBL242004 1 6.75
CHEMBL245231 1 6.70
CHEMBL242003 1 6.00
CHEMBL389129 1 4.47
CHEMBL395788 1 -
CHEMBL245229 1 -
CHEMBL245010 1 -
CHEMBL389128 1 -
CHEMBL244372 1 -
CHEMBL244163 1 -
CHEMBL394569 1 -
CHEMBL244004 1 -
CHEMBL244003 1 -
CHEMBL395789 1 -
CHEMBL243794 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185271 SNAP-7941 Ki = 40.0 nM 7.40
CHEMBL363548 CHLOROHALOPERIDOL Ki = 150.0 nM 6.82
CHEMBL242004 Ki = 180.0 nM 6.75
CHEMBL245231 Ki = 200.0 nM 6.70
CHEMBL242003 Ki = 1010.0 nM 6.00
CHEMBL389129 Ki = 34000.0 nM 4.47
CHEMBL395788 Ki - -
CHEMBL245229 Ki - -
CHEMBL245010 Ki - -
CHEMBL389128 Ki - -
CHEMBL244372 Ki - -
CHEMBL244163 Ki - -
CHEMBL394569 Ki - -
CHEMBL244004 Ki - -
CHEMBL244003 Ki - -
CHEMBL395789 Ki - -
CHEMBL243794 Ki - -