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Assay Detail

CHEMBL3619484

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

Binding
Inhibition of ERCC1-XPF (unknown origin) by high-throughput fluorescence based in-vitro endonuclease assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

N-Hydroxyimides and hydroxypyrimidinones as inhibitors of the DNA repair complex ERCC1-XPF.
Chapman TM, Wallace C, Gillen KJ, Bakrania P, Khurana P, Coombs PJ, Fox S, Bureau EA, Brownlees J, Melton DW, Saxty B.
Bioorg Med Chem Lett (2015) 25 : 4104 -4108
PubMed 26321360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 5.38 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3617281 1 6.30
CHEMBL3617205 1 6.22
CHEMBL3617209 1 6.22
CHEMBL3617207 1 6.16
CHEMBL3617284 1 6.16
CHEMBL3617286 1 6.10
CHEMBL3617282 1 6.10
CHEMBL3617283 1 6.10
CHEMBL223338 1 6.00
CHEMBL3617285 1 6.00
CHEMBL182381 1 5.82
CHEMBL3617203 1 5.82
CHEMBL3617287 1 5.77
CHEMBL361011 1 5.75
CHEMBL3617206 1 5.57
CHEMBL181653 1 5.54
CHEMBL361350 1 5.41
CHEMBL3617197 1 5.41
CHEMBL440562 1 5.41
CHEMBL216874 1 5.38
CHEMBL3617208 1 5.34
CHEMBL3617199 1 5.21
CHEMBL3617288 1 5.20
CHEMBL3617200 1 5.19
CHEMBL3617201 1 5.18
CHEMBL3617291 1 5.16
CHEMBL3617289 1 5.08
CHEMBL3617198 1 5.04
CHEMBL1415852 1 4.92
CHEMBL3617204 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3617281 IC50 = 500.0 nM 6.30
CHEMBL3617205 IC50 = 600.0 nM 6.22
CHEMBL3617209 IC50 = 600.0 nM 6.22
CHEMBL3617207 IC50 = 700.0 nM 6.16
CHEMBL3617284 IC50 = 700.0 nM 6.16
CHEMBL3617286 IC50 = 800.0 nM 6.10
CHEMBL3617282 IC50 = 800.0 nM 6.10
CHEMBL3617283 IC50 = 800.0 nM 6.10
CHEMBL223338 IC50 = 1000.0 nM 6.00
CHEMBL3617285 IC50 = 1000.0 nM 6.00
CHEMBL3617203 IC50 = 1500.0 nM 5.82
CHEMBL182381 IC50 = 1500.0 nM 5.82
CHEMBL3617287 IC50 = 1700.0 nM 5.77
CHEMBL361011 IC50 = 1800.0 nM 5.75
CHEMBL3617206 IC50 = 2700.0 nM 5.57
CHEMBL181653 IC50 = 2900.0 nM 5.54
CHEMBL361350 IC50 = 3900.0 nM 5.41
CHEMBL3617197 IC50 = 3900.0 nM 5.41
CHEMBL440562 IC50 = 3900.0 nM 5.41
CHEMBL216874 IC50 = 4200.0 nM 5.38
CHEMBL3617208 IC50 = 4600.0 nM 5.34
CHEMBL3617199 IC50 = 6100.0 nM 5.21
CHEMBL3617288 IC50 = 6300.0 nM 5.20
CHEMBL3617200 IC50 = 6400.0 nM 5.19
CHEMBL3617201 IC50 = 6600.0 nM 5.18
CHEMBL3617291 IC50 = 6900.0 nM 5.16
CHEMBL3617289 IC50 = 8400.0 nM 5.08
CHEMBL3617198 IC50 = 9100.0 nM 5.04
CHEMBL1415852 IC50 = 12000.0 nM 4.92
CHEMBL3617204 IC50 = 16400.0 nM 4.79
CHEMBL183852 IC50 = 18100.0 nM 4.74
CHEMBL3617290 IC50 = 25300.0 nM 4.60
CHEMBL187010 IC50 = 27300.0 nM 4.56
CHEMBL1207029 IC50 = 30000.0 nM 4.52
CHEMBL366051 IC50 = 48800.0 nM 4.31
CHEMBL182974 IC50 = 80400.0 nM 4.09
CHEMBL3617202 IC50 = 96200.0 nM 4.02
CHEMBL183018 IC50 > 100000.0 nM -