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Assay Detail

CHEMBL979539

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

Binding
Binding affinity to adrenergic alpha1 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Recent advances in selective alpha1-adrenoreceptor antagonists as antihypertensive agents.
Jain KS, Bariwal JB, Kathiravan MK, Phoujdar MS, Sahne RS, Chauhan BS, Shah AK, Yadav MR.
Bioorg Med Chem (2008) 16 : 4759 -4800
PubMed 18378462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.54 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 1 9.49
CHEMBL90588 1 9.49
CHEMBL25554 1 9.27
CHEMBL54 HALOPERIDOL 4.0 1 9.00
CHEMBL514848 1 8.85
CHEMBL42 CLOZAPINE 4.0 1 8.85
CHEMBL92380 1 6.85
CHEMBL454149 1 6.51
CHEMBL10085 MAZAPERTINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.32 nM 9.49
CHEMBL90588 Ki = 0.32 nM 9.49
CHEMBL25554 Ki = 0.54 nM 9.27
CHEMBL54 HALOPERIDOL Ki = 1.0 nM 9.00
CHEMBL514848 Ki = 1.4 nM 8.85
CHEMBL42 CLOZAPINE Ki = 1.4 nM 8.85
CHEMBL92380 Ki = 140.0 nM 6.85
CHEMBL454149 Ki = 310.0 nM 6.51
CHEMBL10085 MAZAPERTINE Ki < 4.0 nM -