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Assay Detail

CHEMBL3096356

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

Binding
Inhibition of C-Raf (unknown origin) assessed as phosphorylation of MEK1 after 45 mins by TR-FRET assay
22
Total Activities
22
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

RAF proto-oncogene serine/threonine-protein kinase (CHEMBL1906)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Hyohdoh I, Furuichi N, Aoki T, Itezono Y, Shirai H, Ozawa S, Watanabe F, Matsushita M, Sakaitani M, Ho PS, Takanashi K, Harada N, Tomii Y, Yoshinari K, Ori K, Tabo M, Aoki Y, Shimma N, Iikura H.
ACS Med Chem Lett (2013) 4 : 1059 -1063
PubMed 24900605 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.85 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3086065 1 8.10
CHEMBL3092191 1 8.10
CHEMBL3092185 1 7.89
CHEMBL3092195 1 7.64
CHEMBL3092178 1 7.60
CHEMBL3092181 1 7.26
CHEMBL3092176 1 7.20
CHEMBL3092180 1 7.16
CHEMBL3092179 1 7.11
CHEMBL3092193 1 6.92
CHEMBL3092187 1 6.92
CHEMBL3092186 1 6.75
CHEMBL3092188 1 6.66
CHEMBL3092189 1 6.52
CHEMBL3092182 1 6.28
CHEMBL3092183 1 6.08
CHEMBL3092184 1 5.96
CHEMBL3092196 1 5.82
CHEMBL3092190 1 5.62
CHEMBL3092177 1 5.44
CHEMBL3092192 1 -
CHEMBL3092194 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3086065 IC50 = 8.0 nM 8.10
CHEMBL3092191 IC50 = 8.0 nM 8.10
CHEMBL3092185 IC50 = 13.0 nM 7.89
CHEMBL3092195 IC50 = 23.0 nM 7.64
CHEMBL3092178 IC50 = 25.0 nM 7.60
CHEMBL3092181 IC50 = 55.0 nM 7.26
CHEMBL3092176 IC50 = 63.0 nM 7.20
CHEMBL3092180 IC50 = 70.0 nM 7.16
CHEMBL3092179 IC50 = 78.0 nM 7.11
CHEMBL3092193 IC50 = 120.0 nM 6.92
CHEMBL3092187 IC50 = 120.0 nM 6.92
CHEMBL3092186 IC50 = 180.0 nM 6.75
CHEMBL3092188 IC50 = 220.0 nM 6.66
CHEMBL3092189 IC50 = 300.0 nM 6.52
CHEMBL3092182 IC50 = 530.0 nM 6.28
CHEMBL3092183 IC50 = 830.0 nM 6.08
CHEMBL3092184 IC50 = 1100.0 nM 5.96
CHEMBL3092196 IC50 = 1500.0 nM 5.82
CHEMBL3092190 IC50 = 2400.0 nM 5.62
CHEMBL3092177 IC50 = 3600.0 nM 5.44
CHEMBL3092192 IC50 - -
CHEMBL3092194 IC50 > 10000.0 nM -