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Assay Detail

CHEMBL832425

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

Binding
Inhibitory concentration against the xeroderma pigmentosum G
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

DNA excision repair protein ERCC-5 (CHEMBL4736)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.
Tumey LN, Bom D, Huck B, Gleason E, Wang J, Silver D, Brunden K, Boozer S, Rundlett S, Sherf B, Murphy S, Dent T, Leventhal C, Bailey A, Harrington J, Bennani YL.
Bioorg Med Chem Lett (2005) 15 : 277 -281
PubMed 15603939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 9.47 10.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL361962 1 10.64
CHEMBL361011 1 10.55
CHEMBL183133 1 10.21
CHEMBL359533 1 10.21
CHEMBL361350 1 10.00
CHEMBL182381 1 9.89
CHEMBL364591 1 9.87
CHEMBL183792 1 9.84
CHEMBL183852 1 9.80
CHEMBL362842 1 9.80
CHEMBL182687 1 9.73
CHEMBL183062 1 9.70
CHEMBL185325 1 9.67
CHEMBL181962 1 9.65
CHEMBL359747 1 9.64
CHEMBL360615 1 9.59
CHEMBL181766 1 9.59
CHEMBL183539 1 9.56
CHEMBL361546 1 9.54
CHEMBL180566 1 9.48
CHEMBL185322 1 9.26
CHEMBL182077 1 9.26
CHEMBL182974 1 8.70
CHEMBL182519 1 8.52
CHEMBL181709 1 8.40
CHEMBL181637 1 8.34
CHEMBL362205 1 8.07
CHEMBL181907 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL361962 IC50 = 0.023 nM 10.64
CHEMBL361011 IC50 = 0.028 nM 10.55
CHEMBL183133 IC50 = 0.061 nM 10.21
CHEMBL359533 IC50 = 0.062 nM 10.21
CHEMBL361350 IC50 = 0.101 nM 10.00
CHEMBL182381 IC50 = 0.128 nM 9.89
CHEMBL364591 IC50 = 0.136 nM 9.87
CHEMBL183792 IC50 = 0.145 nM 9.84
CHEMBL183852 IC50 = 0.16 nM 9.80
CHEMBL362842 IC50 = 0.157 nM 9.80
CHEMBL182687 IC50 = 0.185 nM 9.73
CHEMBL183062 IC50 = 0.202 nM 9.70
CHEMBL185325 IC50 = 0.215 nM 9.67
CHEMBL181962 IC50 = 0.226 nM 9.65
CHEMBL359747 IC50 = 0.23 nM 9.64
CHEMBL360615 IC50 = 0.258 nM 9.59
CHEMBL181766 IC50 = 0.257 nM 9.59
CHEMBL183539 IC50 = 0.276 nM 9.56
CHEMBL361546 IC50 = 0.292 nM 9.54
CHEMBL180566 IC50 = 0.327 nM 9.48
CHEMBL185322 IC50 = 0.55 nM 9.26
CHEMBL182077 IC50 = 0.556 nM 9.26
CHEMBL182974 IC50 = 2.0 nM 8.70
CHEMBL182519 IC50 = 3.04 nM 8.52
CHEMBL181709 IC50 = 3.99 nM 8.40
CHEMBL181637 IC50 = 4.62 nM 8.34
CHEMBL362205 IC50 = 8.45 nM 8.07
CHEMBL181907 IC50 = 30.2 nM 7.52