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Assay Detail

CHEMBL1025517

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Binding
Inhibition of CSF1R
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Macrophage colony-stimulating factor 1 receptor (CHEMBL1844)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile.
Scott DA, Bell KJ, Campbell CT, Cook DJ, Dakin LA, Del Valle DJ, Drew L, Gero TW, Hattersley MM, Omer CA, Tyurin B, Zheng X.
Bioorg Med Chem Lett (2009) 19 : 701 -705
PubMed 19114305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.82 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481423 1 8.70
CHEMBL481223 1 8.52
CHEMBL481401 1 8.52
CHEMBL480445 1 8.22
CHEMBL481806 1 8.22
CHEMBL480457 1 8.10
CHEMBL480618 1 7.96
CHEMBL480617 1 7.64
CHEMBL519924 1 7.62
CHEMBL479847 1 7.60
CHEMBL481596 1 7.27
CHEMBL480456 1 7.23
CHEMBL481400 1 6.96
CHEMBL521407 1 6.89
CHEMBL481008 1 -
CHEMBL480250 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481423 IC50 = 2.0 nM 8.70
CHEMBL481223 IC50 = 3.0 nM 8.52
CHEMBL481401 IC50 = 3.0 nM 8.52
CHEMBL480445 IC50 = 6.0 nM 8.22
CHEMBL481806 IC50 = 6.0 nM 8.22
CHEMBL480457 IC50 = 8.0 nM 8.10
CHEMBL480618 IC50 = 11.0 nM 7.96
CHEMBL480617 IC50 = 23.0 nM 7.64
CHEMBL519924 IC50 = 24.0 nM 7.62
CHEMBL479847 IC50 = 25.0 nM 7.60
CHEMBL481596 IC50 = 54.0 nM 7.27
CHEMBL480456 IC50 = 59.0 nM 7.23
CHEMBL481400 IC50 = 110.0 nM 6.96
CHEMBL521407 IC50 = 129.0 nM 6.89
CHEMBL481008 IC50 < 3.0 nM -
CHEMBL480250 IC50 < 3.0 nM -