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Assay Detail

CHEMBL4012481

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

Binding
Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay
25
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 11B2, mitochondrial (CHEMBL2722)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures.
Meguro M, Miyauchi S, Kanao Y, Naito S, Suzuki K, Inoue S, Yamada K, Homma T, Chiba K, Nara F, Furuzono S.
Bioorg Med Chem Lett (2017) 27 : 1902 -1906
PubMed 28359792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.88 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4088766 1 9.40
CHEMBL4082403 3 9.14
CHEMBL4070323 1 8.70
CHEMBL4070230 1 8.70
CHEMBL4091167 1 8.52
CHEMBL4099824 1 8.52
CHEMBL287677 DEXFADROSTAT 2.0 1 8.40
CHEMBL4093575 1 8.30
CHEMBL4072943 1 8.30
CHEMBL4097020 1 8.15
CHEMBL4061565 1 8.10
CHEMBL4092081 1 8.10
CHEMBL4064367 1 7.85
CHEMBL4079006 1 7.82
CHEMBL4065476 1 7.52
CHEMBL4072871 1 7.32
CHEMBL4104118 1 7.12
CHEMBL4083387 1 7.08
CHEMBL4067686 1 6.96
CHEMBL4075207 1 6.84
CHEMBL4101118 1 6.72
CHEMBL4077051 1 6.52
CHEMBL4060559 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4088766 IC50 = 0.4 nM 9.40
CHEMBL4082403 IC50 = 0.73 nM 9.14
CHEMBL4070323 IC50 = 2.0 nM 8.70
CHEMBL4070230 IC50 = 2.0 nM 8.70
CHEMBL4091167 IC50 = 3.0 nM 8.52
CHEMBL4099824 IC50 = 3.0 nM 8.52
CHEMBL4082403 IC50 = 4.0 nM 8.40
CHEMBL287677 DEXFADROSTAT IC50 = 4.0 nM 8.40
CHEMBL4072943 IC50 = 5.0 nM 8.30
CHEMBL4093575 IC50 = 5.0 nM 8.30
CHEMBL4097020 IC50 = 7.0 nM 8.15
CHEMBL4061565 IC50 = 8.0 nM 8.10
CHEMBL4092081 IC50 = 8.0 nM 8.10
CHEMBL4064367 IC50 = 14.0 nM 7.85
CHEMBL4079006 IC50 = 15.0 nM 7.82
CHEMBL4065476 IC50 = 30.0 nM 7.52
CHEMBL4072871 IC50 = 48.0 nM 7.32
CHEMBL4104118 IC50 = 75.0 nM 7.12
CHEMBL4083387 IC50 = 83.0 nM 7.08
CHEMBL4067686 IC50 = 109.0 nM 6.96
CHEMBL4075207 IC50 = 144.0 nM 6.84
CHEMBL4101118 IC50 = 192.0 nM 6.72
CHEMBL4060559 IC50 = 300.0 nM 6.52
CHEMBL4077051 IC50 = 300.0 nM 6.52
CHEMBL4082403 IC50 > 100.0 nM -