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Assay Detail

CHEMBL4030905

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

Binding
Inhibition of human BRPF1 (627 to 740 residues) expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay
34
Total Activities
34
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

Peregrin (CHEMBL3132741)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV.
J Med Chem (2017) 60 : 6998 -7011
PubMed 28714688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.00 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752151 1 8.51
CHEMBL4102050 1 8.10
CHEMBL4069814 1 8.05
CHEMBL4105505 1 7.92
CHEMBL4103077 1 7.92
CHEMBL4059962 1 7.82
CHEMBL4087315 1 7.77
CHEMBL4061727 1 7.62
CHEMBL4084805 1 7.54
CHEMBL4079434 1 7.41
CHEMBL4076056 1 7.37
CHEMBL4068981 1 7.28
CHEMBL4102751 1 7.28
CHEMBL4103693 1 7.26
CHEMBL4103432 1 7.25
CHEMBL4067436 1 7.19
CHEMBL4073708 1 7.03
CHEMBL4064071 1 7.00
CHEMBL4064386 1 6.96
CHEMBL4085921 1 6.80
CHEMBL4065116 1 6.77
CHEMBL4080511 1 6.75
CHEMBL4067917 1 6.60
CHEMBL4094867 1 6.42
CHEMBL4070377 1 6.37
CHEMBL4078346 1 6.28
CHEMBL4086558 1 6.06
CHEMBL4095325 1 6.04
CHEMBL4072276 1 6.00
CHEMBL4090059 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752151 IC50 = 3.1 nM 8.51
CHEMBL4102050 IC50 = 7.9 nM 8.10
CHEMBL4069814 IC50 = 9.0 nM 8.05
CHEMBL4105505 IC50 = 12.0 nM 7.92
CHEMBL4103077 IC50 = 12.0 nM 7.92
CHEMBL4059962 IC50 = 15.0 nM 7.82
CHEMBL4087315 IC50 = 17.0 nM 7.77
CHEMBL4061727 IC50 = 24.0 nM 7.62
CHEMBL4084805 IC50 = 29.0 nM 7.54
CHEMBL4079434 IC50 = 39.0 nM 7.41
CHEMBL4076056 IC50 = 43.0 nM 7.37
CHEMBL4068981 IC50 = 52.0 nM 7.28
CHEMBL4102751 IC50 = 53.0 nM 7.28
CHEMBL4103693 IC50 = 55.0 nM 7.26
CHEMBL4103432 IC50 = 56.0 nM 7.25
CHEMBL4067436 IC50 = 65.0 nM 7.19
CHEMBL4073708 IC50 = 93.0 nM 7.03
CHEMBL4064071 IC50 = 100.0 nM 7.00
CHEMBL4064386 IC50 = 110.0 nM 6.96
CHEMBL4085921 IC50 = 160.0 nM 6.80
CHEMBL4065116 IC50 = 170.0 nM 6.77
CHEMBL4080511 IC50 = 180.0 nM 6.75
CHEMBL4067917 IC50 = 250.0 nM 6.60
CHEMBL4094867 IC50 = 380.0 nM 6.42
CHEMBL4070377 IC50 = 430.0 nM 6.37
CHEMBL4078346 IC50 = 520.0 nM 6.28
CHEMBL4086558 IC50 = 870.0 nM 6.06
CHEMBL4095325 IC50 = 910.0 nM 6.04
CHEMBL4072276 IC50 = 1000.0 nM 6.00
CHEMBL4090059 IC50 = 1000.0 nM 6.00
CHEMBL4102614 IC50 = 1100.0 nM 5.96
CHEMBL4086220 IC50 = 1200.0 nM 5.92
CHEMBL4064729 IC50 = 2200.0 nM 5.66
CHEMBL4059509 IC50 > 100000.0 nM -