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Assay Detail

CHEMBL4774696

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

Functional
Antagonist activity at human alpha1D receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The one-pot synthesis of butyl-1H-indol-3-alkylcarboxylic acid derivatives in ionic liquid as potent dual-acting agent for management of BPH.
Zeng LY,Yang F,Chen K,Zeng Y,Jiang Z,Liu S,Xi B
Eur J Med Chem (2020) 205 : 112616 -112616
PubMed 32949920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.16 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL836 TAMSULOSIN 4.0 1 9.82
CHEMBL4797460 1 6.79
CHEMBL4797051 1 6.72
CHEMBL4792905 1 6.72
CHEMBL4788144 1 6.48
CHEMBL4785526 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL836 TAMSULOSIN IC50 = 0.15 nM 9.82
CHEMBL4797460 IC50 = 163.6 nM 6.79
CHEMBL4797051 IC50 = 188.7 nM 6.72
CHEMBL4792905 IC50 = 189.0 nM 6.72
CHEMBL4788144 IC50 = 329.0 nM 6.48
CHEMBL4785526 IC50 = 377.7 nM 6.42