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Assay Detail

CHEMBL3755449

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

Binding
Inhibition of B-Raf V600E mutant (unknown origin) by lantha screen assay
15
Total Activities
15
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

Discovery of EBI-907: A highly potent and orally active B-Raf(V600E) inhibitor for the treatment of melanoma and associated cancers.
Lu B, Cao H, Cao J, Huang S, Hu Q, Liu D, Shen R, Shen X, Tao W, Wan H, Wang D, Yan Y, Yang L, Zhang J, Zhang L, Zhang L, Zhang M.
Bioorg Med Chem Lett (2016) 26 : 819 -823
PubMed 26739779 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.06 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752213 1 10.00
CHEMBL3753260 1 9.22
CHEMBL3754618 1 9.10
CHEMBL3752762 1 9.10
CHEMBL3752478 1 8.15
CHEMBL3751896 1 8.15
CHEMBL2023335 1 8.06
CHEMBL3752457 1 7.96
CHEMBL3753363 1 7.77
CHEMBL3751892 1 7.70
CHEMBL3753663 1 7.16
CHEMBL3753972 1 7.10
CHEMBL3753129 1 6.66
CHEMBL1230020 PLX-4720 1 6.66
CHEMBL3754116 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752213 IC50 = 0.1 nM 10.00
CHEMBL3753260 IC50 = 0.6 nM 9.22
CHEMBL3754618 IC50 = 0.8 nM 9.10
CHEMBL3752762 IC50 = 0.8 nM 9.10
CHEMBL3752478 IC50 = 7.0 nM 8.15
CHEMBL3751896 IC50 = 7.0 nM 8.15
CHEMBL2023335 IC50 = 8.7 nM 8.06
CHEMBL3752457 IC50 = 11.0 nM 7.96
CHEMBL3753363 IC50 = 17.0 nM 7.77
CHEMBL3751892 IC50 = 20.0 nM 7.70
CHEMBL3753663 IC50 = 70.0 nM 7.16
CHEMBL3753972 IC50 = 80.0 nM 7.10
CHEMBL3753129 IC50 = 220.0 nM 6.66
CHEMBL1230020 PLX-4720 IC50 = 220.0 nM 6.66
CHEMBL3754116 IC50 > 30.0 nM -