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Assay Detail

CHEMBL3405641

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

Binding
Antagonist activity at alpha-1B adrenergic receptor (unknown origin) incubated for 30 mins prior to agonist addition measured after 5 hrs by CCF4-AM staining-based cellular assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Alpha-1B adrenergic receptor (CHEMBL232)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

α-Adrenoceptor antagonistic and hypotensive properties of novel arylpiperazine derivatives of pyrrolidin-2-one.
Zaręba P, Dudek M, Lustyk K, Siwek A, Starowicz G, Bednarski M, Nowiński L, Raźny K, Sapa J, Malawska B, Kulig K.
Bioorg Med Chem (2015) 23 : 2104 -2111
PubMed 25813897 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.70 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL611 TERAZOSIN 4.0 1 9.30
CHEMBL3400597 1 8.60
CHEMBL3400593 1 8.46
CHEMBL3400596 1 7.33
CHEMBL3400594 1 6.88
CHEMBL3400595 1 6.78
CHEMBL3400598 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL611 TERAZOSIN EC50 = 0.5 nM 9.30
CHEMBL3400597 EC50 = 2.53 nM 8.60
CHEMBL3400593 EC50 = 3.5 nM 8.46
CHEMBL3400596 EC50 = 46.9 nM 7.33
CHEMBL3400594 EC50 = 131.1 nM 6.88
CHEMBL3400595 EC50 = 165.3 nM 6.78
CHEMBL3400598 EC50 = 288.7 nM 6.54