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Assay Detail

CHEMBL766737

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Binding
Inhibitory concentration against raf kinase.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery of heterocyclic ureas as a new class of raf kinase inhibitors: identification of a second generation lead by a combinatorial chemistry approach.
Smith RA, Barbosa J, Blum CL, Bobko MA, Caringal YV, Dally R, Johnson JS, Katz ME, Kennure N, Kingery-Wood J, Lee W, Lowinger TB, Lyons J, Marsh V, Rogers DH, Swartz S, Walling T, Wild H.
Bioorg Med Chem Lett (2001) 11 : 2775 -2778
PubMed 11591521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.23 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1794051 1 8.05
CHEMBL94487 1 6.27
CHEMBL317839 1 5.92
CHEMBL279377 1 5.77
CHEMBL96793 1 5.72
CHEMBL328143 1 5.70
CHEMBL278719 1 5.52
CHEMBL18764 1 5.52
CHEMBL94879 1 5.51
CHEMBL317611 1 5.43
CHEMBL18848 1 5.40
CHEMBL18754 1 5.31
CHEMBL275580 1 5.22
CHEMBL96383 1 5.22
CHEMBL316315 1 5.18
CHEMBL96536 1 5.17
CHEMBL278737 1 5.17
CHEMBL93264 1 5.12
CHEMBL278057 1 5.11
CHEMBL96077 1 5.10
CHEMBL93185 1 5.09
CHEMBL92721 1 4.96
CHEMBL328854 1 4.96
CHEMBL328572 1 4.96
CHEMBL317305 1 4.92
CHEMBL317109 1 4.92
CHEMBL92934 1 4.89
CHEMBL94156 1 4.82
CHEMBL279560 1 4.82
CHEMBL96260 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1794051 IC50 = 9.0 nM 8.05
CHEMBL94487 IC50 = 540.0 nM 6.27
CHEMBL317839 IC50 = 1200.0 nM 5.92
CHEMBL279377 IC50 = 1700.0 nM 5.77
CHEMBL96793 IC50 = 1900.0 nM 5.72
CHEMBL328143 IC50 = 2000.0 nM 5.70
CHEMBL278719 IC50 = 3000.0 nM 5.52
CHEMBL18764 IC50 = 3000.0 nM 5.52
CHEMBL94879 IC50 = 3100.0 nM 5.51
CHEMBL317611 IC50 = 3700.0 nM 5.43
CHEMBL18848 IC50 = 4000.0 nM 5.40
CHEMBL18754 IC50 = 4900.0 nM 5.31
CHEMBL275580 IC50 = 6000.0 nM 5.22
CHEMBL96383 IC50 = 6000.0 nM 5.22
CHEMBL316315 IC50 = 6600.0 nM 5.18
CHEMBL96536 IC50 = 6700.0 nM 5.17
CHEMBL278737 IC50 = 6800.0 nM 5.17
CHEMBL93264 IC50 = 7600.0 nM 5.12
CHEMBL278057 IC50 = 7700.0 nM 5.11
CHEMBL96077 IC50 = 8000.0 nM 5.10
CHEMBL93185 IC50 = 8100.0 nM 5.09
CHEMBL92721 IC50 = 11000.0 nM 4.96
CHEMBL328854 IC50 = 11000.0 nM 4.96
CHEMBL328572 IC50 = 11000.0 nM 4.96
CHEMBL317305 IC50 = 12000.0 nM 4.92
CHEMBL317109 IC50 = 12000.0 nM 4.92
CHEMBL92934 IC50 = 13000.0 nM 4.89
CHEMBL279560 IC50 = 15000.0 nM 4.82
CHEMBL96260 IC50 = 15000.0 nM 4.82
CHEMBL94156 IC50 = 15000.0 nM 4.82
CHEMBL95114 IC50 = 16000.0 nM 4.80
CHEMBL19148 IC50 = 17000.0 nM 4.77
CHEMBL18942 IC50 = 18000.0 nM 4.75
CHEMBL329079 IC50 = 19000.0 nM 4.72
CHEMBL94581 IC50 = 20000.0 nM 4.70
CHEMBL318248 IC50 = 20000.0 nM 4.70
CHEMBL321312 IC50 = 22000.0 nM 4.66