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Assay Detail

CHEMBL2428261

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Binding
Inhibition of BLM (unknown origin) by gel-based DNA unwinding assay
ChEMBL ↗
57
Total Activities
57
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

Target

RecQ-like DNA helicase BLM (CHEMBL1293237) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.
Rosenthal AS, Dexheimer TS, Gileadi O, Nguyen GH, Chu WK, Hickson ID, Jadhav A, Simeonov A, Maloney DJ.
Bioorg Med Chem Lett (2013) 23 : 5660 -5666
PubMed 24012121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 5.29 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2426190 — — 1 7.00
CHEMBL2426164 — — 1 6.96
CHEMBL2426169 — — 1 6.52
CHEMBL2426165 — — 1 6.04
CHEMBL2426174 — — 1 5.96
CHEMBL2426193 — — 1 5.89
CHEMBL1321933 — — 1 5.85
CHEMBL2426195 — — 1 5.80
CHEMBL2426177 — — 1 5.75
CHEMBL2426168 — — 1 5.75
CHEMBL2426161 — — 1 5.68
CHEMBL2426159 — — 1 5.50
CHEMBL2426200 — — 1 5.46
CHEMBL2426179 — — 1 5.40
CHEMBL2426181 — — 1 5.40
CHEMBL2426187 — — 1 5.37
CHEMBL2426160 — — 1 5.25
CHEMBL2426192 — — 1 5.15
CHEMBL2426196 — — 1 5.10
CHEMBL2426191 — — 1 5.10
CHEMBL2426197 — — 1 5.05
CHEMBL2426166 — — 1 5.05
CHEMBL2426176 — — 1 5.00
CHEMBL2426194 — — 1 4.95
CHEMBL2426162 — — 1 4.90
CHEMBL2426163 — — 1 4.87
CHEMBL1428264 — — 1 4.85
CHEMBL2426175 — — 1 4.85
CHEMBL2426172 — — 1 4.85
CHEMBL2426182 — — 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2426190 — IC50 = 100.0 nM 7.00
CHEMBL2426164 — IC50 = 110.0 nM 6.96
CHEMBL2426169 — IC50 = 300.0 nM 6.52
CHEMBL2426165 — IC50 = 910.0 nM 6.04
CHEMBL2426174 — IC50 = 1100.0 nM 5.96
CHEMBL2426193 — IC50 = 1300.0 nM 5.89
CHEMBL1321933 — IC50 = 1400.0 nM 5.85
CHEMBL2426195 — IC50 = 1600.0 nM 5.80
CHEMBL2426177 — IC50 = 1800.0 nM 5.75
CHEMBL2426168 — IC50 = 1800.0 nM 5.75
CHEMBL2426161 — IC50 = 2100.0 nM 5.68
CHEMBL2426159 — IC50 = 3200.0 nM 5.50
CHEMBL2426200 — IC50 = 3500.0 nM 5.46
CHEMBL2426181 — IC50 = 4000.0 nM 5.40
CHEMBL2426179 — IC50 = 4000.0 nM 5.40
CHEMBL2426187 — IC50 = 4300.0 nM 5.37
CHEMBL2426160 — IC50 = 5600.0 nM 5.25
CHEMBL2426192 — IC50 = 7100.0 nM 5.15
CHEMBL2426196 — IC50 = 7900.0 nM 5.10
CHEMBL2426191 — IC50 = 7900.0 nM 5.10
CHEMBL2426197 — IC50 = 8900.0 nM 5.05
CHEMBL2426166 — IC50 = 8900.0 nM 5.05
CHEMBL2426176 — IC50 = 10000.0 nM 5.00
CHEMBL2426194 — IC50 = 11200.0 nM 4.95
CHEMBL2426162 — IC50 = 12600.0 nM 4.90
CHEMBL2426163 — IC50 = 13400.0 nM 4.87
CHEMBL2426175 — IC50 = 14200.0 nM 4.85
CHEMBL2426172 — IC50 = 14100.0 nM 4.85
CHEMBL2426182 — IC50 = 14100.0 nM 4.85
CHEMBL1428264 — IC50 = 14100.0 nM 4.85
CHEMBL2426167 — IC50 = 15800.0 nM 4.80
CHEMBL2426173 — IC50 = 16800.0 nM 4.78
CHEMBL2426207 — IC50 = 28100.0 nM 4.55
CHEMBL2426171 — IC50 = 36000.0 nM 4.44
CHEMBL1488371 — IC50 = 40000.0 nM 4.40
CHEMBL2426170 — IC50 = 40000.0 nM 4.40
CHEMBL2426202 — IC50 = 49000.0 nM 4.31
CHEMBL2426211 — IC50 - — -
CHEMBL2426188 — IC50 - — -
CHEMBL2426209 — IC50 - — -
CHEMBL2426208 — IC50 - — -
CHEMBL2426206 — IC50 - — -
CHEMBL2426205 — IC50 - — -
CHEMBL2426204 — IC50 - — -
CHEMBL2426203 — IC50 - — -
CHEMBL2426201 — IC50 - — -
CHEMBL2426199 — IC50 - — -
CHEMBL2426198 — IC50 - — -
CHEMBL2426210 — IC50 - — -
CHEMBL2426189 — IC50 - — -