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Assay Detail

CHEMBL700452

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

Functional
Tested for the inhibition of 20-HETE production from arachidonic acid (AA) by human renal microsomes
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 1 — Organism
Curated By Expert

Target

Homo sapiens (CHEMBL372)
Type ORGANISM
Organism Homo sapiens

Publication

Discovery of a N'-hydroxyphenylformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor.
Sato M, Ishii T, Kobayashi-Matsunaga Y, Amada H, Taniguchi K, Miyata N, Kameo K.
Bioorg Med Chem Lett (2001) 11 : 2993 -2995
PubMed 11714595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.14 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101180 1 8.62
CHEMBL100899 1 8.52
CHEMBL317798 1 8.46
CHEMBL103313 1 8.41
CHEMBL321051 1 8.31
CHEMBL101296 1 8.18
CHEMBL103163 1 8.11
CHEMBL267865 1 8.05
CHEMBL445120 1 7.28
CHEMBL103320 1 6.17
CHEMBL319862 1 6.14
CHEMBL102906 1 6.12
CHEMBL319772 1 5.73
CHEMBL103168 1 5.48
CHEMBL103651 1 5.44
CHEMBL99906 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101180 IC50 = 2.4 nM 8.62
CHEMBL100899 IC50 = 3.0 nM 8.52
CHEMBL317798 IC50 = 3.5 nM 8.46
CHEMBL103313 IC50 = 3.9 nM 8.41
CHEMBL321051 IC50 = 4.9 nM 8.31
CHEMBL101296 IC50 = 6.6 nM 8.18
CHEMBL103163 IC50 = 7.8 nM 8.11
CHEMBL267865 IC50 = 8.9 nM 8.05
CHEMBL445120 IC50 = 52.0 nM 7.28
CHEMBL103320 IC50 = 669.0 nM 6.17
CHEMBL319862 IC50 = 720.0 nM 6.14
CHEMBL102906 IC50 = 759.0 nM 6.12
CHEMBL319772 IC50 = 1845.0 nM 5.73
CHEMBL103168 IC50 = 3286.0 nM 5.48
CHEMBL103651 IC50 = 3625.0 nM 5.44
CHEMBL99906 IC50 = 6812.0 nM 5.17