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Assay Detail

CHEMBL2317019

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Binding
Inhibition of human Flag-tagged LEDGF interaction to His6-tagged HIV1 integrase expressed in Escherichia coli BL21 (DE3) preincubated for 20 mins measured after 1 hr by AlphaScreen proximity luminescent assay
ChEMBL ↗
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Discovery of novel inhibitors of LEDGF/p75-IN protein-protein interactions.
Sanchez TW, Debnath B, Christ F, Otake H, Debyser Z, Neamati N.
Bioorg Med Chem (2013) 21 : 957 -963
PubMed 23306052 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 4.93 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL569410 — — 1 6.40
CHEMBL2311867 — — 1 5.89
CHEMBL2311872 — — 1 5.70
CHEMBL2311897 — — 1 5.70
CHEMBL2311893 — — 1 5.52
CHEMBL2311902 — — 1 5.52
CHEMBL199592 — — 1 5.40
CHEMBL200144 — — 1 5.40
CHEMBL2311873 — — 1 5.40
CHEMBL2311874 — — 1 5.40
CHEMBL2311885 — — 1 5.30
CHEMBL1597979 — — 1 5.22
CHEMBL390195 — — 1 5.22
CHEMBL2311887 — — 1 5.22
CHEMBL3145360 — — 1 5.22
CHEMBL2311903 — — 1 5.22
CHEMBL2311890 — — 1 5.22
CHEMBL2094455 — — 1 5.16
CHEMBL2311881 — — 1 5.10
CHEMBL2311911 — — 1 5.10
CHEMBL2311898 — — 1 4.92
CHEMBL2311882 — — 1 4.89
CHEMBL2311889 — — 1 4.89
CHEMBL2311910 — — 1 4.85
CHEMBL2094513 — — 1 4.80
CHEMBL2311906 — — 1 4.72
CHEMBL2311896 — — 1 4.70
CHEMBL1489980 — — 1 4.68
CHEMBL1976649 — — 1 4.68
CHEMBL2311912 — — 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL569410 — IC50 = 400.0 nM 6.40
CHEMBL2311867 — IC50 = 1300.0 nM 5.89
CHEMBL2311897 — IC50 = 2000.0 nM 5.70
CHEMBL2311872 — IC50 = 2000.0 nM 5.70
CHEMBL2311893 — IC50 = 3000.0 nM 5.52
CHEMBL2311902 — IC50 = 3000.0 nM 5.52
CHEMBL199592 — IC50 = 4000.0 nM 5.40
CHEMBL200144 — IC50 = 4000.0 nM 5.40
CHEMBL2311873 — IC50 = 4000.0 nM 5.40
CHEMBL2311874 — IC50 = 4000.0 nM 5.40
CHEMBL2311885 — IC50 = 5000.0 nM 5.30
CHEMBL2311887 — IC50 = 6000.0 nM 5.22
CHEMBL390195 — IC50 = 6000.0 nM 5.22
CHEMBL1597979 — IC50 = 6000.0 nM 5.22
CHEMBL3145360 — IC50 = 6000.0 nM 5.22
CHEMBL2311903 — IC50 = 6000.0 nM 5.22
CHEMBL2311890 — IC50 = 6000.0 nM 5.22
CHEMBL2094455 — IC50 = 7000.0 nM 5.16
CHEMBL2311881 — IC50 = 8000.0 nM 5.10
CHEMBL2311911 — IC50 = 8000.0 nM 5.10
CHEMBL2311898 — IC50 = 12000.0 nM 4.92
CHEMBL2311882 — IC50 = 13000.0 nM 4.89
CHEMBL2311889 — IC50 = 13000.0 nM 4.89
CHEMBL2311910 — IC50 = 14000.0 nM 4.85
CHEMBL2094513 — IC50 = 16000.0 nM 4.80
CHEMBL2311906 — IC50 = 19000.0 nM 4.72
CHEMBL2311896 — IC50 = 20000.0 nM 4.70
CHEMBL1489980 — IC50 = 21000.0 nM 4.68
CHEMBL1976649 — IC50 = 21000.0 nM 4.68
CHEMBL2311912 — IC50 = 23000.0 nM 4.64
CHEMBL2311905 — IC50 = 24000.0 nM 4.62
CHEMBL2311891 — IC50 = 25000.0 nM 4.60
CHEMBL2311908 — IC50 = 32000.0 nM 4.50
CHEMBL2311909 — IC50 = 34000.0 nM 4.47
CHEMBL2311904 — IC50 = 35000.0 nM 4.46
CHEMBL2311899 — IC50 = 36000.0 nM 4.44
CHEMBL2311877 — IC50 = 38000.0 nM 4.42
CHEMBL2311900 — IC50 = 39000.0 nM 4.41
CHEMBL2311894 — IC50 = 40000.0 nM 4.40
CHEMBL2311895 — IC50 = 46000.0 nM 4.34
CHEMBL2311878 — IC50 = 50000.0 nM 4.30
CHEMBL2311879 — IC50 = 50000.0 nM 4.30
CHEMBL2311880 — IC50 = 50000.0 nM 4.30
CHEMBL2311907 — IC50 = 50000.0 nM 4.30
CHEMBL2311864 — IC50 = 93000.0 nM 4.03
CHEMBL2311901 — IC50 > 50000.0 nM -
CHEMBL2311913 — IC50 < 25000.0 nM -
CHEMBL2311865 — IC50 > 50000.0 nM -
CHEMBL2311866 — IC50 > 50000.0 nM -
CHEMBL2311868 — IC50 > 50000.0 nM -