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Assay Detail

CHEMBL3240201

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

Binding
Inhibition of full-length B-Raf V600E mutant (unknown origin)
24
Total Activities
24
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

Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J.
Bioorg Med Chem Lett (2014) 24 : 1923 -1927
PubMed 24675381 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.19 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3236470 1 9.70
CHEMBL3236463 1 9.70
CHEMBL3236471 1 9.70
CHEMBL3236472 1 9.52
CHEMBL3236464 1 9.52
CHEMBL2144069 1 9.22
CHEMBL3236198 1 8.70
CHEMBL3236459 1 8.70
CHEMBL3233047 1 8.52
CHEMBL3236193 1 8.40
CHEMBL3236467 1 8.10
CHEMBL3236196 1 7.96
CHEMBL3236466 1 7.96
CHEMBL3236462 1 7.92
CHEMBL3236195 1 7.80
CHEMBL3236460 1 7.77
CHEMBL3236461 1 7.72
CHEMBL3236194 1 7.60
CHEMBL3236468 1 7.58
CHEMBL3236469 1 7.52
CHEMBL3236192 1 7.48
CHEMBL3236197 1 7.00
CHEMBL3236191 1 6.50
CHEMBL3236465 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3236470 IC50 = 0.2 nM 9.70
CHEMBL3236463 IC50 = 0.2 nM 9.70
CHEMBL3236471 IC50 = 0.2 nM 9.70
CHEMBL3236472 IC50 = 0.3 nM 9.52
CHEMBL3236464 IC50 = 0.3 nM 9.52
CHEMBL2144069 IC50 = 0.6 nM 9.22
CHEMBL3236198 IC50 = 2.0 nM 8.70
CHEMBL3236459 IC50 = 2.0 nM 8.70
CHEMBL3233047 IC50 = 3.0 nM 8.52
CHEMBL3236193 IC50 = 4.0 nM 8.40
CHEMBL3236467 IC50 = 8.0 nM 8.10
CHEMBL3236196 IC50 = 11.0 nM 7.96
CHEMBL3236466 IC50 = 11.0 nM 7.96
CHEMBL3236462 IC50 = 12.0 nM 7.92
CHEMBL3236195 IC50 = 16.0 nM 7.80
CHEMBL3236460 IC50 = 17.0 nM 7.77
CHEMBL3236461 IC50 = 19.0 nM 7.72
CHEMBL3236194 IC50 = 25.0 nM 7.60
CHEMBL3236468 IC50 = 26.0 nM 7.58
CHEMBL3236469 IC50 = 30.0 nM 7.52
CHEMBL3236192 IC50 = 33.0 nM 7.48
CHEMBL3236197 IC50 = 100.0 nM 7.00
CHEMBL3236191 IC50 = 314.0 nM 6.50
CHEMBL3236465 IC50 = 851.0 nM 6.07