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Assay Detail

CHEMBL4124009

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

Binding
Inhibition of recombinant CYP17 (unknown origin) expressed in human AD293 cells using [21-3H]17alpha-hydroxypregnenolone as substrate preincubated for 60 mins followed by substrate addition measured after 4 hrs Topcount method
34
Total Activities
34
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

Steroid 17-alpha-hydroxylase/17,20 lyase (CHEMBL3522)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of functionalized piperazin-1yl-(E)-stilbenes as inhibitors of 17α-hydroxylase-C17,20-lyase (Cyp17).
Blass BE, Iyer P, Abou-Gharbia M, Childers WE, Gordon JC, Ramanjulu M, Morton G, Arumugam P, Boruwa J, Ellingboe J, Mitra S, Reddy Nimmareddy R, Paliwal S, Rajasekhar J, Shivakumar S, Srivastava P, Tangirala RS, Venkataramanaiah K, Bobbala R, Yanamandra M, Krishnakanth Reddy L.
Bioorg Med Chem Lett (2018) 28 : 2270 -2274
PubMed 29803730 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.79 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127656 1 9.00
CHEMBL4126996 1 9.00
CHEMBL4128368 1 8.70
CHEMBL4129721 1 8.34
CHEMBL4126284 1 8.30
CHEMBL4128640 1 8.30
CHEMBL4127256 1 8.30
CHEMBL4126014 1 8.30
CHEMBL4127399 1 8.30
CHEMBL4129859 1 8.30
CHEMBL4126429 1 8.30
CHEMBL4127131 1 8.30
CHEMBL4126956 1 8.30
CHEMBL4126816 1 8.30
CHEMBL4129428 1 8.30
CHEMBL4128495 1 8.22
CHEMBL4127240 1 8.21
CHEMBL4128621 1 7.77
CHEMBL4128197 1 7.75
CHEMBL4127385 1 7.68
CHEMBL4128449 1 7.62
CHEMBL4125765 1 7.47
CHEMBL4127378 1 7.41
CHEMBL4127969 1 7.38
CHEMBL4129703 1 7.38
CHEMBL157101 KETOCONAZOLE 4.0 1 7.32
CHEMBL4125996 1 7.24
CHEMBL4125902 1 7.07
CHEMBL4129210 1 7.00
CHEMBL4129355 1 6.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127656 IC50 = 1.0 nM 9.00
CHEMBL4126996 IC50 = 1.0 nM 9.00
CHEMBL4128368 IC50 = 2.0 nM 8.70
CHEMBL4129721 IC50 = 4.6 nM 8.34
CHEMBL4126284 IC50 = 5.0 nM 8.30
CHEMBL4128640 IC50 = 5.0 nM 8.30
CHEMBL4127256 IC50 = 5.0 nM 8.30
CHEMBL4126014 IC50 = 5.0 nM 8.30
CHEMBL4127399 IC50 = 5.0 nM 8.30
CHEMBL4129859 IC50 = 5.0 nM 8.30
CHEMBL4126429 IC50 = 5.0 nM 8.30
CHEMBL4127131 IC50 = 5.0 nM 8.30
CHEMBL4126956 IC50 = 5.0 nM 8.30
CHEMBL4126816 IC50 = 5.0 nM 8.30
CHEMBL4129428 IC50 = 5.0 nM 8.30
CHEMBL4128495 IC50 = 6.0 nM 8.22
CHEMBL4127240 IC50 = 6.2 nM 8.21
CHEMBL4128621 IC50 = 17.0 nM 7.77
CHEMBL4128197 IC50 = 18.0 nM 7.75
CHEMBL4127385 IC50 = 21.0 nM 7.68
CHEMBL4128449 IC50 = 24.0 nM 7.62
CHEMBL4125765 IC50 = 34.0 nM 7.47
CHEMBL4127378 IC50 = 39.0 nM 7.41
CHEMBL4127969 IC50 = 42.0 nM 7.38
CHEMBL4129703 IC50 = 42.0 nM 7.38
CHEMBL157101 KETOCONAZOLE IC50 = 48.0 nM 7.32
CHEMBL4125996 IC50 = 58.0 nM 7.24
CHEMBL4125902 IC50 = 86.0 nM 7.07
CHEMBL4129210 IC50 = 100.0 nM 7.00
CHEMBL4129355 IC50 = 117.0 nM 6.93
CHEMBL4126412 IC50 = 180.0 nM 6.75
CHEMBL4126731 IC50 = 1200.0 nM 5.92
CHEMBL4128105 IC50 = 2500.0 nM 5.60
CHEMBL4130227 IC50 = 17.0 nM -