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Assay Detail

CHEMBL4257178

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

Binding
Inhibition of recombinant CYP21 (unknown origin) expressed in human AD293 cells using 17alpha-hydroxyprogesterone as substrate pretreated for 60 mins followed by substrate addition and measured after 45 mins by LC/MS analysis
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Steroid 21-hydroxylase (CHEMBL2759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel cytochrome p450 inhibitors and their method of use
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 5.76 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4284756 1 7.14
CHEMBL4279221 1 7.07
CHEMBL4287787 1 6.80
CHEMBL4127656 1 6.72
CHEMBL4291002 1 6.60
CHEMBL4279727 1 6.54
CHEMBL4128368 1 6.50
CHEMBL4127385 1 6.47
CHEMBL4126996 1 6.41
CHEMBL4128640 1 6.38
CHEMBL4129721 1 6.37
CHEMBL4288457 1 6.31
CHEMBL4126284 1 6.28
CHEMBL4288256 1 6.28
CHEMBL4128449 1 6.27
CHEMBL4127256 1 6.25
CHEMBL4279416 1 6.23
CHEMBL4127378 1 6.16
CHEMBL4126429 1 6.13
CHEMBL4286910 1 6.11
CHEMBL4126014 1 6.08
CHEMBL4283570 1 6.07
CHEMBL4127969 1 6.00
CHEMBL4283402 1 6.00
CHEMBL4289268 1 6.00
CHEMBL4127399 1 5.96
CHEMBL4289969 1 5.92
CHEMBL4129428 1 5.92
CHEMBL4126816 1 5.92
CHEMBL4292267 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4284756 IC50 = 73.0 nM 7.14
CHEMBL4279221 IC50 = 85.0 nM 7.07
CHEMBL4287787 IC50 = 160.0 nM 6.80
CHEMBL4127656 IC50 = 190.0 nM 6.72
CHEMBL4291002 IC50 = 250.0 nM 6.60
CHEMBL4279727 IC50 = 285.0 nM 6.54
CHEMBL4128368 IC50 = 316.0 nM 6.50
CHEMBL4127385 IC50 = 340.0 nM 6.47
CHEMBL4126996 IC50 = 393.0 nM 6.41
CHEMBL4128640 IC50 = 416.0 nM 6.38
CHEMBL4129721 IC50 = 430.0 nM 6.37
CHEMBL4288457 IC50 = 490.0 nM 6.31
CHEMBL4126284 IC50 = 520.0 nM 6.28
CHEMBL4288256 IC50 = 520.0 nM 6.28
CHEMBL4128449 IC50 = 540.0 nM 6.27
CHEMBL4127256 IC50 = 565.0 nM 6.25
CHEMBL4279416 IC50 = 585.0 nM 6.23
CHEMBL4127378 IC50 = 700.0 nM 6.16
CHEMBL4126429 IC50 = 740.0 nM 6.13
CHEMBL4286910 IC50 = 770.0 nM 6.11
CHEMBL4126014 IC50 = 840.0 nM 6.08
CHEMBL4283570 IC50 = 850.0 nM 6.07
CHEMBL4127969 IC50 = 1000.0 nM 6.00
CHEMBL4283402 IC50 = 1010.0 nM 6.00
CHEMBL4289268 IC50 = 1000.0 nM 6.00
CHEMBL4127399 IC50 = 1100.0 nM 5.96
CHEMBL4129428 IC50 = 1200.0 nM 5.92
CHEMBL4126816 IC50 = 1200.0 nM 5.92
CHEMBL4292267 IC50 = 1200.0 nM 5.92
CHEMBL4289969 IC50 = 1200.0 nM 5.92
CHEMBL4128621 IC50 = 1380.0 nM 5.86
CHEMBL4280777 IC50 = 1400.0 nM 5.85
CHEMBL4285546 IC50 = 1600.0 nM 5.80
CHEMBL4280985 IC50 = 1950.0 nM 5.71
CHEMBL4126412 IC50 = 2200.0 nM 5.66
CHEMBL4282398 IC50 = 2400.0 nM 5.62
CHEMBL4283084 IC50 = 2400.0 nM 5.62
CHEMBL4284598 IC50 = 2600.0 nM 5.58
CHEMBL4280378 IC50 = 2800.0 nM 5.55
CHEMBL4286077 IC50 = 2870.0 nM 5.54
CHEMBL4288168 IC50 = 3300.0 nM 5.48
CHEMBL4282697 IC50 = 3300.0 nM 5.48
CHEMBL4129210 IC50 = 3500.0 nM 5.46
CHEMBL4287119 IC50 = 10000.0 nM 5.00
CHEMBL4288241 IC50 = 10000.0 nM 5.00
CHEMBL4279912 IC50 = 10000.0 nM 5.00
CHEMBL4281653 IC50 = 10000.0 nM 5.00
CHEMBL4285301 IC50 = 10000.0 nM 5.00
CHEMBL4288970 IC50 = 10000.0 nM 5.00
CHEMBL4283190 IC50 = 10000.0 nM 5.00