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Assay Detail

CHEMBL3591373

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

Binding
Binding affinity to FLAG-6His-Tev-ATAD2 (950 to 1148) (unknown origin) expressed in Escherichia coli BL21 (DE3) by SPR analysis
16
Total Activities
7
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
Kd 16 6.36 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3590391 2 7.30
CHEMBL3590405 2 7.22
CHEMBL3590383 2 7.10
CHEMBL3590408 2 6.70
CHEMBL3590396 2 6.00
CHEMBL3590388 4 5.64
CHEMBL3590394 2 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3590391 Kd = 50.0 nM 7.30
CHEMBL3590391 Kd = 50.12 nM 7.30
CHEMBL3590405 Kd = 60.0 nM 7.22
CHEMBL3590405 Kd = 63.1 nM 7.20
CHEMBL3590383 Kd = 79.43 nM 7.10
CHEMBL3590383 Kd = 90.0 nM 7.05
CHEMBL3590408 Kd = 200.0 nM 6.70
CHEMBL3590408 Kd = 199.53 nM 6.70
CHEMBL3590396 Kd = 1000.0 nM 6.00
CHEMBL3590396 Kd = 1100.0 nM 5.96
CHEMBL3590388 Kd = 2300.0 nM 5.64
CHEMBL3590388 Kd = 2511.89 nM 5.60
CHEMBL3590388 Kd = 2900.0 nM 5.54
CHEMBL3590388 Kd = 3162.28 nM 5.50
CHEMBL3590394 Kd = 3200.0 nM 5.50
CHEMBL3590394 Kd = 3162.28 nM 5.50