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Assay Detail

CHEMBL4036596

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

Binding
Inhibition of human ERG
15
Total Activities
15
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

Publication

Novel 3-fluoro-6-methoxyquinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.
Mitton-Fry MJ, Brickner SJ, Hamel JC, Barham R, Brennan L, Casavant JM, Ding X, Finegan S, Hardink J, Hoang T, Huband MD, Maloney M, Marfat A, McCurdy SP, McLeod D, Subramanyam C, Plotkin M, Reilly U, Schafer J, Stone GG, Uccello DP, Wisialowski T, Yoon K, Zaniewski R, Zook C.
Bioorg Med Chem Lett (2017) 27 : 3353 -3358
PubMed 28610977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.59 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2382345 1 5.00
CHEMBL4082602 1 4.97
CHEMBL4097890 1 4.85
CHEMBL2159976 1 4.71
CHEMBL4103746 1 4.65
CHEMBL2158050 1 4.63
CHEMBL4079869 1 4.60
CHEMBL2382287 1 4.60
CHEMBL4078201 1 4.35
CHEMBL4064317 1 4.34
CHEMBL2382343 1 4.32
CHEMBL4092041 1 4.07
CHEMBL4101570 1 -
CHEMBL2424928 1 -
CHEMBL3317856 GEPOTIDACIN 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2382345 IC50 = 9970.0 nM 5.00
CHEMBL4082602 IC50 = 10700.0 nM 4.97
CHEMBL4097890 IC50 = 14100.0 nM 4.85
CHEMBL2159976 IC50 = 19700.0 nM 4.71
CHEMBL4103746 IC50 = 22300.0 nM 4.65
CHEMBL2158050 IC50 = 23600.0 nM 4.63
CHEMBL4079869 IC50 = 25000.0 nM 4.60
CHEMBL2382287 IC50 = 24900.0 nM 4.60
CHEMBL4078201 IC50 = 45000.0 nM 4.35
CHEMBL4064317 IC50 = 45300.0 nM 4.34
CHEMBL2382343 IC50 = 47600.0 nM 4.32
CHEMBL4092041 IC50 = 85900.0 nM 4.07
CHEMBL4101570 IC50 > 300000.0 nM -
CHEMBL2424928 IC50 > 300000.0 nM -
CHEMBL3317856 GEPOTIDACIN IC50 = 588.0 ug.mL-1 -