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Assay Detail

CHEMBL4397121

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

Binding
Inhibition of C-terminal GST-tagged human SET1B (1629 to 1923 amino acids) expressed in Escherichia coli using core histone as substrate in presence of WDR5 (22 to 334 amino acids),RbBP5 (1 to 538 amino acids),Ash2L (2 to 534 amino acids),DPY-30 (1 to 99 amino acids) by fluorescence method
1
Total Activities
1
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

Histone-lysine N-methyltransferase SETD1B (CHEMBL4105837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
Nguyen W, Jacobson J, Jarman KE, Jousset Sabroux H, Harty L, McMahon J, Lewin SR, Purcell DF, Sleebs BE.
J Med Chem (2019) 62 : 5148 -5175
PubMed 30973727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.85 4.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465202 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465202 IC50 = 14000.0 nM 4.85