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Assay Detail

CHEMBL829355

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

Binding
Concentration required for 50% inhibition of Flap endonuclease-1
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Flap endonuclease 1 (CHEMBL5027)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
Tumey LN, Huck B, Gleason E, Wang J, Silver D, Brunden K, Boozer S, Rundlett S, Sherf B, Murphy S, Bailey A, Dent T, Leventhal C, Harrington J, Bennani YL.
Bioorg Med Chem Lett (2004) 14 : 4915 -4918
PubMed 15341951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 5.24 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182748 1 6.72
CHEMBL188067 1 6.48
CHEMBL183257 1 6.39
CHEMBL182756 1 6.36
CHEMBL361960 1 6.24
CHEMBL185652 1 5.87
CHEMBL367585 1 5.82
CHEMBL440938 1 5.78
CHEMBL185721 1 5.76
CHEMBL187154 1 5.74
CHEMBL274003 1 5.46
CHEMBL363721 1 5.46
CHEMBL185787 1 5.44
CHEMBL186926 1 5.26
CHEMBL184215 1 5.16
CHEMBL186181 1 5.14
CHEMBL182485 1 5.12
CHEMBL183604 1 5.00
CHEMBL183027 1 4.97
CHEMBL361460 1 4.95
CHEMBL185257 1 4.91
CHEMBL185898 1 4.89
CHEMBL185566 1 4.87
CHEMBL364328 1 4.84
CHEMBL185879 1 4.75
CHEMBL424806 1 4.71
CHEMBL19332 1 4.60
CHEMBL364984 1 4.54
CHEMBL361807 1 4.46
CHEMBL185070 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182748 IC50 = 190.0 nM 6.72
CHEMBL188067 IC50 = 330.0 nM 6.48
CHEMBL183257 IC50 = 410.0 nM 6.39
CHEMBL182756 IC50 = 440.0 nM 6.36
CHEMBL361960 IC50 = 570.0 nM 6.24
CHEMBL185652 IC50 = 1360.0 nM 5.87
CHEMBL367585 IC50 = 1520.0 nM 5.82
CHEMBL440938 IC50 = 1660.0 nM 5.78
CHEMBL185721 IC50 = 1750.0 nM 5.76
CHEMBL187154 IC50 = 1820.0 nM 5.74
CHEMBL274003 IC50 = 3500.0 nM 5.46
CHEMBL363721 IC50 = 3510.0 nM 5.46
CHEMBL185787 IC50 = 3620.0 nM 5.44
CHEMBL186926 IC50 = 5530.0 nM 5.26
CHEMBL184215 IC50 = 6960.0 nM 5.16
CHEMBL186181 IC50 = 7310.0 nM 5.14
CHEMBL182485 IC50 = 7650.0 nM 5.12
CHEMBL183604 IC50 = 10100.0 nM 5.00
CHEMBL183027 IC50 = 10800.0 nM 4.97
CHEMBL361460 IC50 = 11300.0 nM 4.95
CHEMBL185257 IC50 = 12200.0 nM 4.91
CHEMBL185898 IC50 = 12900.0 nM 4.89
CHEMBL185566 IC50 = 13500.0 nM 4.87
CHEMBL364328 IC50 = 14500.0 nM 4.84
CHEMBL185879 IC50 = 17700.0 nM 4.75
CHEMBL424806 IC50 = 19300.0 nM 4.71
CHEMBL19332 IC50 = 24900.0 nM 4.60
CHEMBL364984 IC50 = 29000.0 nM 4.54
CHEMBL361807 IC50 = 34300.0 nM 4.46
CHEMBL185070 IC50 = 37900.0 nM 4.42
CHEMBL182129 IC50 = 46400.0 nM 4.33
CHEMBL181810 IC50 = 63200.0 nM 4.20
CHEMBL177529 IC50 = 64200.0 nM 4.19
CHEMBL181811 IC50 > 100000.0 nM -
CHEMBL361338 IC50 > 100000.0 nM -
CHEMBL182290 IC50 > 100000.0 nM -