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Assay Detail

CHEMBL869914

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

Binding
Binding affinity at bRaf kinase in fluorescent ligand displacement assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Serine/threonine-protein kinase B-raf (CHEMBL5145)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification of potent and selective imidazole-based inhibitors of B-Raf kinase.
Takle AK, Brown MJ, Davies S, Dean DK, Francis G, Gaiba A, Hird AW, King FD, Lovell PJ, Naylor A, Reith AD, Steadman JG, Wilson DM.
Bioorg Med Chem Lett (2006) 16 : 378 -381
PubMed 16260133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 30 7.92 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477989 SB590885 1 9.52
CHEMBL372543 1 8.89
CHEMBL200172 1 8.70
CHEMBL373011 1 8.62
CHEMBL371952 1 8.38
CHEMBL200889 1 8.32
CHEMBL200783 1 8.30
CHEMBL200320 1 8.28
CHEMBL200258 1 8.24
CHEMBL200412 1 8.22
CHEMBL304624 1 8.10
CHEMBL381447 1 8.00
CHEMBL200637 1 7.96
CHEMBL370353 1 7.85
CHEMBL200164 1 7.77
CHEMBL200863 1 7.68
CHEMBL427196 1 7.66
CHEMBL426476 1 7.62
CHEMBL200942 1 7.57
CHEMBL200118 1 7.41
CHEMBL200431 1 7.28
CHEMBL200226 1 7.15
CHEMBL381421 1 7.06
CHEMBL435744 1 6.88
CHEMBL68215 1 6.50
CHEMBL200156 1 -
CHEMBL200782 1 -
CHEMBL200861 1 -
CHEMBL305023 1 -
CHEMBL200259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477989 SB590885 Kd = 0.3 nM 9.52
CHEMBL372543 Kd = 1.3 nM 8.89
CHEMBL200172 Kd = 2.0 nM 8.70
CHEMBL373011 Kd = 2.4 nM 8.62
CHEMBL371952 Kd = 4.2 nM 8.38
CHEMBL200889 Kd = 4.8 nM 8.32
CHEMBL200783 Kd = 5.0 nM 8.30
CHEMBL200320 Kd = 5.3 nM 8.28
CHEMBL200258 Kd = 5.7 nM 8.24
CHEMBL200412 Kd = 6.0 nM 8.22
CHEMBL304624 Kd = 8.0 nM 8.10
CHEMBL381447 Kd = 10.0 nM 8.00
CHEMBL200637 Kd = 11.0 nM 7.96
CHEMBL370353 Kd = 14.0 nM 7.85
CHEMBL200164 Kd = 17.0 nM 7.77
CHEMBL200863 Kd = 21.0 nM 7.68
CHEMBL427196 Kd = 22.0 nM 7.66
CHEMBL426476 Kd = 24.0 nM 7.62
CHEMBL200942 Kd = 27.0 nM 7.57
CHEMBL200118 Kd = 39.0 nM 7.41
CHEMBL200431 Kd = 53.0 nM 7.28
CHEMBL200226 Kd = 71.0 nM 7.15
CHEMBL381421 Kd = 87.0 nM 7.06
CHEMBL435744 Kd = 132.0 nM 6.88
CHEMBL68215 Kd = 316.0 nM 6.50
CHEMBL200156 Kd > 200.0 nM -
CHEMBL200782 Kd > 200.0 nM -
CHEMBL200861 Kd > 200.0 nM -
CHEMBL305023 Kd > 196.0 nM -
CHEMBL200259 Kd > 196.0 nM -