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Assay Detail

CHEMBL4050071

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Binding
Inhibition of recombinant human N-terminal GST-tagged BRAF catalytic domain (416 to 766 residues) V600E mutant expressed in baculovirus expression system using human His6-tagged MEK1 K97R mutant as substrate pretreated for 20 mins followed by [33P]-ATP addition measured after 2 hrs by filter binding method
ChEMBL ↗
59
Total Activities
59
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

Design, synthesis and evaluation of derivatives based on pyrimidine scaffold as potent Pan-Raf inhibitors to overcome resistance.
Wang L, Zhang Q, Zhu G, Zhang Z, Zhi Y, Zhang L, Mao T, Zhou X, Chen Y, Lu T, Tang W.
Eur J Med Chem (2017) 130 : 86 -106
PubMed 28242553 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 7.42 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061139 — — 1 9.52
CHEMBL4060057 — — 1 8.55
CHEMBL4073430 — — 1 8.37
CHEMBL4071785 — — 1 8.08
CHEMBL4075036 — — 1 7.91
CHEMBL4101717 — — 1 7.86
CHEMBL4085294 — — 1 7.84
CHEMBL4093166 — — 1 7.74
CHEMBL4087837 — — 1 7.73
CHEMBL4098457 — — 1 7.73
CHEMBL4082425 — — 1 7.71
CHEMBL4080362 — — 1 7.69
CHEMBL4082762 — — 1 7.67
CHEMBL4063679 — — 1 7.67
CHEMBL4072281 — — 1 7.65
CHEMBL4060531 — — 1 7.63
CHEMBL4066939 — — 1 7.62
CHEMBL4066903 — — 1 7.60
CHEMBL4104590 — — 1 7.58
CHEMBL4077908 — — 1 7.54
CHEMBL4082943 — — 1 7.51
CHEMBL1229517 VEMURAFENIB 4.0 1 7.50
CHEMBL4103293 — — 1 7.50
CHEMBL4079029 — — 1 7.45
CHEMBL1336 SORAFENIB 4.0 1 7.42
CHEMBL4069743 — — 1 7.41
CHEMBL4061063 — — 1 7.41
CHEMBL4095541 — — 1 7.37
CHEMBL4096093 — — 1 7.36
CHEMBL4068793 — — 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061139 — IC50 = 0.3 nM 9.52
CHEMBL4060057 — IC50 = 2.8 nM 8.55
CHEMBL4073430 — IC50 = 4.3 nM 8.37
CHEMBL4071785 — IC50 = 8.4 nM 8.08
CHEMBL4075036 — IC50 = 12.2 nM 7.91
CHEMBL4101717 — IC50 = 13.9 nM 7.86
CHEMBL4085294 — IC50 = 14.3 nM 7.84
CHEMBL4093166 — IC50 = 18.3 nM 7.74
CHEMBL4087837 — IC50 = 18.7 nM 7.73
CHEMBL4098457 — IC50 = 18.5 nM 7.73
CHEMBL4082425 — IC50 = 19.5 nM 7.71
CHEMBL4080362 — IC50 = 20.5 nM 7.69
CHEMBL4082762 — IC50 = 21.6 nM 7.67
CHEMBL4063679 — IC50 = 21.4 nM 7.67
CHEMBL4072281 — IC50 = 22.4 nM 7.65
CHEMBL4060531 — IC50 = 23.4 nM 7.63
CHEMBL4066939 — IC50 = 24.1 nM 7.62
CHEMBL4066903 — IC50 = 25.1 nM 7.60
CHEMBL4104590 — IC50 = 26.5 nM 7.58
CHEMBL4077908 — IC50 = 29.1 nM 7.54
CHEMBL4082943 — IC50 = 30.8 nM 7.51
CHEMBL1229517 VEMURAFENIB IC50 = 31.6 nM 7.50
CHEMBL4103293 — IC50 = 31.5 nM 7.50
CHEMBL4079029 — IC50 = 35.8 nM 7.45
CHEMBL1336 SORAFENIB IC50 = 38.1 nM 7.42
CHEMBL4069743 — IC50 = 38.6 nM 7.41
CHEMBL4061063 — IC50 = 39.1 nM 7.41
CHEMBL4095541 — IC50 = 43.1 nM 7.37
CHEMBL4096093 — IC50 = 44.1 nM 7.36
CHEMBL4068793 — IC50 = 46.1 nM 7.34
CHEMBL4069812 — IC50 = 59.5 nM 7.22
CHEMBL4059496 — IC50 = 68.2 nM 7.17
CHEMBL4101882 — IC50 = 77.2 nM 7.11
CHEMBL4079957 — IC50 = 80.2 nM 7.10
CHEMBL4088215 — IC50 = 88.6 nM 7.05
CHEMBL4062173 — IC50 = 135.0 nM 6.87
CHEMBL4068160 — IC50 = 140.0 nM 6.85
CHEMBL4074595 — IC50 = 145.0 nM 6.84
CHEMBL4090806 — IC50 = 143.0 nM 6.84
CHEMBL4090742 — IC50 = 152.0 nM 6.82
CHEMBL4095947 — IC50 = 178.0 nM 6.75
CHEMBL4083018 — IC50 = 201.0 nM 6.70
CHEMBL4103699 — IC50 = 237.0 nM 6.62
CHEMBL4099453 — IC50 = 251.0 nM 6.60
CHEMBL4092569 — IC50 = 388.0 nM 6.41
CHEMBL4072537 — IC50 = 441.0 nM 6.36
CHEMBL4073524 — IC50 - — -
CHEMBL4096391 — IC50 - — -
CHEMBL4100362 — IC50 - — -
CHEMBL4064929 — IC50 - — -