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Assay Detail

CHEMBL4730989

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

Binding
Inhibition of BRD4 in human HEL cells harboring JAK2 V617F mutant assessed as decrease in metabolic activity measured after 72 hrs by MTT assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEL
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies.
Altenburg B,Frings M,Schöbel JH,Goßen J,Pannen K,Vanderliek K,Rossetti G,Koschmieder S,Chatain N,Bolm C
ACS Med Chem Lett (2020) 11 : 1928 -1934
PubMed 33062175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.00 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790505 1 6.30
CHEMBL2179387 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790505 IC50 = 500.0 nM 6.30
CHEMBL2179387 IC50 = 2000.0 nM 5.70