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Assay Detail

CHEMBL995611

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

ADMET
Inhibition of CYP3A4
27
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and orally bioavailable zwitterion GnRH antagonists with low CYP3A4 inhibitory activity.
Chen C, Chen Y, Pontillo J, Guo Z, Huang CQ, Wu D, Madan A, Chen T, Wen J, Xie Q, Tucci FC, Rowbottom M, Zhu YF, Wade W, Saunders J, Bozigian H, Struthers RS.
Bioorg Med Chem Lett (2008) 18 : 3301 -3305
PubMed 18442910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.68 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL508435 1 7.32
CHEMBL434936 1 7.00
CHEMBL499026 1 6.92
CHEMBL445691 1 6.89
CHEMBL189164 1 6.80
CHEMBL371613 1 6.75
CHEMBL365985 1 6.52
CHEMBL503624 1 6.46
CHEMBL364914 1 6.42
CHEMBL192172 1 6.36
CHEMBL455769 1 6.29
CHEMBL191817 1 6.22
CHEMBL499307 1 6.17
CHEMBL495882 1 6.10
CHEMBL497747 1 5.04
CHEMBL499589 1 4.80
CHEMBL450471 2 4.80
CHEMBL499588 1 4.70
CHEMBL526887 1 4.70
CHEMBL456279 1 4.51
CHEMBL526327 1 4.48
CHEMBL499849 1 4.44
CHEMBL509075 2 4.44
CHEMBL508020 1 4.32
CHEMBL453167 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL508435 IC50 = 48.0 nM 7.32
CHEMBL434936 IC50 = 100.0 nM 7.00
CHEMBL499026 IC50 = 120.0 nM 6.92
CHEMBL445691 IC50 = 130.0 nM 6.89
CHEMBL189164 IC50 = 160.0 nM 6.80
CHEMBL371613 IC50 = 180.0 nM 6.75
CHEMBL365985 IC50 = 300.0 nM 6.52
CHEMBL503624 IC50 = 350.0 nM 6.46
CHEMBL364914 IC50 = 380.0 nM 6.42
CHEMBL192172 IC50 = 440.0 nM 6.36
CHEMBL455769 IC50 = 510.0 nM 6.29
CHEMBL191817 IC50 = 600.0 nM 6.22
CHEMBL499307 IC50 = 670.0 nM 6.17
CHEMBL495882 IC50 = 800.0 nM 6.10
CHEMBL497747 IC50 = 9100.0 nM 5.04
CHEMBL450471 IC50 = 15848.93 nM 4.80
CHEMBL499589 IC50 = 16000.0 nM 4.80
CHEMBL450471 IC50 = 17000.0 nM 4.77
CHEMBL499588 IC50 = 20000.0 nM 4.70
CHEMBL526887 IC50 = 20000.0 nM 4.70
CHEMBL456279 IC50 = 31000.0 nM 4.51
CHEMBL526327 IC50 = 33000.0 nM 4.48
CHEMBL499849 IC50 = 36000.0 nM 4.44
CHEMBL509075 IC50 = 36000.0 nM 4.44
CHEMBL509075 IC50 = 39810.72 nM 4.40
CHEMBL508020 IC50 = 48000.0 nM 4.32
CHEMBL453167 IC50 > 50000.0 nM -