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Assay Detail

CHEMBL4715072

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

Binding
Inhibition of BRAF (unknown origin) (416 to 766) assessed as using inactive phosphorylated MAP2K1 substrate preincubated for 30 mins measured after 90 mins by DELFIA assay
8
Total Activities
8
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

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

Publication

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.
Huestis MP,Durk MR,Eigenbrot C,Gibbons P,Hunsaker TL,La H,Leung DH,Liu W,Malek S,Merchant M,Moffat JG,Muli CS,Orr CJ,Parr BT,Shanahan F,Sneeringer CJ,Wang W,Yen I,Yin J,Rudolph J,Siu M
ACS Med Chem Lett (2021) 12 : 791 -797
PubMed 34055227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.87 9.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4740241 1 9.99
CHEMBL4776565 1 9.92
CHEMBL3577124 LY-3009120 1.0 1 9.86
CHEMBL4778419 1 9.72
CHEMBL4780060 1 -
CHEMBL4775998 1 -
CHEMBL4778772 1 -
CHEMBL4758903 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4740241 Ki = 0.102 nM 9.99
CHEMBL4776565 Ki = 0.12 nM 9.92
CHEMBL3577124 LY-3009120 Ki = 0.139 nM 9.86
CHEMBL4778419 Ki = 0.19 nM 9.72
CHEMBL4780060 Ki < 0.08 nM -
CHEMBL4775998 Ki < 0.08 nM -
CHEMBL4778772 Ki < 0.08 nM -
CHEMBL4758903 Ki < 0.08 nM -