Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4024633

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

ADMET
Inhibition of full length His6-tagged BRAF (unknown origin) expressed in baculovirus expression system assessed as reduction in MEK phosphorylation by measuring ADP production by BRAMA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors.
Philp J, Lawhorn BG, Graves AP, Shewchuk L, Rivera KL, Jolivette LJ, Holt DA, Gatto GJ, Kallander LS.
J Med Chem (2018) 61 : 3076 -3088
PubMed 29561151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.82 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4087038 1 7.89
CHEMBL4102486 1 7.70
CHEMBL4074231 1 6.70
CHEMBL4094739 1 6.60
CHEMBL4070430 1 6.30
CHEMBL4091362 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4087038 IC50 = 13.0 nM 7.89
CHEMBL4102486 IC50 = 20.0 nM 7.70
CHEMBL4074231 IC50 = 200.0 nM 6.70
CHEMBL4094739 IC50 = 250.0 nM 6.60
CHEMBL4070430 IC50 = 500.0 nM 6.30
CHEMBL4091362 IC50 = 2000.0 nM 5.70