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Assay Detail

CHEMBL4828223

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

Binding
Inhibition of HIS9-tagged BPTF (unknown origin) expressed in Escherichia coli BL21 (DE3) cells incubated for 30 mins by AlphaScreen assay
26
Total Activities
26
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

Nucleosome-remodeling factor subunit BPTF (CHEMBL3085621)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New Design Rules for Developing Potent Cell-Active Inhibitors of the Nucleosome Remodeling Factor (NURF) via BPTF Bromodomain Inhibition.
Zahid H, Buchholz CR, Singh M, Ciccone MF, Chan A, Nithianantham S, Shi K, Aihara H, Fischer M, Schönbrunn E, Dos Santos CO, Landry JW, Pomerantz WCK.
J Med Chem (2021) 64 : 13902 -13917
PubMed 34515477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 5.98 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4861491 1 7.44
CHEMBL4848701 1 7.25
CHEMBL4872300 1 7.17
CHEMBL4848138 1 6.77
CHEMBL4101756 1 6.66
CHEMBL4850516 1 6.60
CHEMBL4866748 1 6.54
CHEMBL4870218 1 6.51
CHEMBL4848082 1 6.43
CHEMBL4863631 1 6.42
CHEMBL4877696 1 6.26
CHEMBL4850913 1 6.16
CHEMBL4855881 1 6.10
CHEMBL4863529 1 6.10
CHEMBL4065579 1 6.02
CHEMBL4877118 1 6.01
CHEMBL4069412 1 5.82
CHEMBL4861822 1 5.50
CHEMBL4858548 1 5.41
CHEMBL4872107 1 5.11
CHEMBL4853420 1 5.06
CHEMBL4849136 1 5.00
CHEMBL4867912 1 5.00
CHEMBL4857332 1 4.96
CHEMBL4072538 1 4.72
CHEMBL4871852 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4861491 IC50 = 36.0 nM 7.44
CHEMBL4848701 IC50 = 56.0 nM 7.25
CHEMBL4872300 IC50 = 67.0 nM 7.17
CHEMBL4848138 IC50 = 170.0 nM 6.77
CHEMBL4101756 IC50 = 220.0 nM 6.66
CHEMBL4850516 IC50 = 250.0 nM 6.60
CHEMBL4866748 IC50 = 290.0 nM 6.54
CHEMBL4870218 IC50 = 310.0 nM 6.51
CHEMBL4848082 IC50 = 370.0 nM 6.43
CHEMBL4863631 IC50 = 380.0 nM 6.42
CHEMBL4877696 IC50 = 550.0 nM 6.26
CHEMBL4850913 IC50 = 700.0 nM 6.16
CHEMBL4855881 IC50 = 800.0 nM 6.10
CHEMBL4863529 IC50 = 790.0 nM 6.10
CHEMBL4065579 IC50 = 950.0 nM 6.02
CHEMBL4877118 IC50 = 970.0 nM 6.01
CHEMBL4069412 IC50 = 1500.0 nM 5.82
CHEMBL4861822 IC50 = 3200.0 nM 5.50
CHEMBL4858548 IC50 = 3900.0 nM 5.41
CHEMBL4872107 IC50 = 7700.0 nM 5.11
CHEMBL4853420 IC50 = 8700.0 nM 5.06
CHEMBL4849136 IC50 = 10000.0 nM 5.00
CHEMBL4867912 IC50 = 10000.0 nM 5.00
CHEMBL4857332 IC50 = 11000.0 nM 4.96
CHEMBL4072538 IC50 = 19000.0 nM 4.72
CHEMBL4871852 IC50 = 31000.0 nM 4.51