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Assay Detail

CHEMBL1035690

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

Binding
Inhibition of human cloned wild type BRAF by ELISA-based MEK phosphorylation assay
33
Total Activities
33
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of BRAF inhibitors through in silico screening.
Luo C, Xie P, Marmorstein R.
J Med Chem (2008) 51 : 6121 -6127
PubMed 18783202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 4.91 5.76
Ki 2 8.61 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477989 SB590885 1 9.80
CHEMBL1336 SORAFENIB 4.0 1 7.42
CHEMBL460137 1 5.76
CHEMBL454028 1 5.68
CHEMBL461421 1 5.43
CHEMBL462473 1 5.34
CHEMBL460136 1 4.96
CHEMBL517286 1 4.96
CHEMBL459514 1 4.95
CHEMBL459935 1 4.76
CHEMBL516963 1 4.53
CHEMBL459931 1 4.52
CHEMBL516644 1 4.43
CHEMBL518187 1 4.24
CHEMBL518163 1 4.24
CHEMBL459714 1 -
CHEMBL459500 1 -
CHEMBL460344 1 -
CHEMBL516808 1 -
CHEMBL509283 1 -
CHEMBL461621 1 -
CHEMBL516494 1 -
CHEMBL462280 1 -
CHEMBL462279 1 -
CHEMBL462071 1 -
CHEMBL516655 1 -
CHEMBL459736 1 -
CHEMBL516807 1 -
CHEMBL502945 1 -
CHEMBL459515 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477989 SB590885 Ki = 0.16 nM 9.80
CHEMBL1336 SORAFENIB Ki = 38.0 nM 7.42
CHEMBL460137 IC50 = 1720.0 nM 5.76
CHEMBL454028 IC50 = 2100.0 nM 5.68
CHEMBL461421 IC50 = 3750.0 nM 5.43
CHEMBL462473 IC50 = 4600.0 nM 5.34
CHEMBL460136 IC50 = 10910.0 nM 4.96
CHEMBL517286 IC50 = 11080.0 nM 4.96
CHEMBL459514 IC50 = 11360.0 nM 4.95
CHEMBL459935 IC50 = 17360.0 nM 4.76
CHEMBL516963 IC50 = 29420.0 nM 4.53
CHEMBL459931 IC50 = 30110.0 nM 4.52
CHEMBL516644 IC50 = 37480.0 nM 4.43
CHEMBL518187 IC50 = 57710.0 nM 4.24
CHEMBL518163 IC50 = 57890.0 nM 4.24
CHEMBL459936 IC50 > 50000.0 nM -
CHEMBL462046 IC50 > 100000.0 nM -
CHEMBL459715 IC50 > 100000.0 nM -
CHEMBL459714 IC50 > 100000.0 nM -
CHEMBL459500 IC50 > 100000.0 nM -
CHEMBL460344 IC50 > 100000.0 nM -
CHEMBL516808 IC50 > 100000.0 nM -
CHEMBL509283 IC50 > 100000.0 nM -
CHEMBL461621 IC50 > 100000.0 nM -
CHEMBL516494 IC50 > 100000.0 nM -
CHEMBL462280 IC50 > 100000.0 nM -
CHEMBL462279 IC50 > 100000.0 nM -
CHEMBL462071 IC50 > 100000.0 nM -
CHEMBL516655 IC50 > 100000.0 nM -
CHEMBL459736 IC50 > 100000.0 nM -
CHEMBL516807 IC50 > 100000.0 nM -
CHEMBL502945 IC50 > 100000.0 nM -
CHEMBL459515 IC50 > 100000.0 nM -