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Assay Detail

CHEMBL3591371

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

Binding
Binding affinity to ATAD2 (unknown origin) using HuT-78 chromatin lysate incubated for 2 hrs by bromosphere competition binding assay
18
Total Activities
16
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

ATPase family AAA domain-containing protein 2 (CHEMBL2150837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH.
J Med Chem (2015) 58 : 6151 -6178
PubMed 26230603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.73 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3590383 1 7.50
CHEMBL3590391 1 7.40
CHEMBL3590405 2 7.40
CHEMBL3590407 1 7.30
CHEMBL3590406 1 7.20
CHEMBL3590381 1 7.00
CHEMBL3590385 1 7.00
CHEMBL3590408 1 7.00
CHEMBL3590380 1 6.70
CHEMBL3590382 1 6.60
CHEMBL3590389 1 6.50
CHEMBL3590384 1 6.50
CHEMBL3590396 2 6.30
CHEMBL3590386 1 6.10
CHEMBL3590394 1 5.80
CHEMBL3590388 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3590383 IC50 = 31.62 nM 7.50
CHEMBL3590391 IC50 = 39.81 nM 7.40
CHEMBL3590405 IC50 = 39.81 nM 7.40
CHEMBL3590405 IC50 = 39.81 nM 7.40
CHEMBL3590407 IC50 = 50.12 nM 7.30
CHEMBL3590406 IC50 = 63.1 nM 7.20
CHEMBL3590408 IC50 = 100.0 nM 7.00
CHEMBL3590385 IC50 = 100.0 nM 7.00
CHEMBL3590381 IC50 = 100.0 nM 7.00
CHEMBL3590380 IC50 = 199.53 nM 6.70
CHEMBL3590382 IC50 = 251.19 nM 6.60
CHEMBL3590384 IC50 = 316.23 nM 6.50
CHEMBL3590389 IC50 = 316.23 nM 6.50
CHEMBL3590396 IC50 = 501.19 nM 6.30
CHEMBL3590386 IC50 = 794.33 nM 6.10
CHEMBL3590396 IC50 = 1000.0 nM 6.00
CHEMBL3590394 IC50 = 1584.89 nM 5.80
CHEMBL3590388 IC50 = 3981.07 nM 5.40