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Assay Detail

CHEMBL5342458

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

Binding
Inhibition of CSF1R (530 to 910 residues) (unknown origin)
34
Total Activities
34
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

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

Publication

Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form.
Aarhus TI, Bjørnstad F, Wolowczyk C, Larsen KU, Rognstad L, Leithaug T, Unger A, Habenberger P, Wolf A, Bjørkøy G, Pridans C, Eickhoff J, Klebl B, Hoff BH, Sundby E.
J Med Chem (2023) 66 : 6959 -6980
PubMed 37191268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.57 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5432649 1 9.52
CHEMBL5434318 1 9.52
CHEMBL5417607 1 9.40
CHEMBL5428404 1 9.30
CHEMBL5406924 1 9.30
CHEMBL5417494 1 9.15
CHEMBL5406771 1 9.10
CHEMBL5422465 1 9.10
CHEMBL5431583 1 9.00
CHEMBL5424694 1 9.00
CHEMBL5403478 1 8.96
CHEMBL5395449 1 8.92
CHEMBL5411378 1 8.89
CHEMBL5440766 1 8.77
CHEMBL5439547 1 8.70
CHEMBL5432592 1 8.68
CHEMBL5414964 1 8.62
CHEMBL5426924 1 8.60
CHEMBL5406951 1 8.55
CHEMBL5436096 1 8.55
CHEMBL5417945 1 8.55
CHEMBL5418474 1 8.43
CHEMBL5438430 1 8.43
CHEMBL5411522 1 8.28
CHEMBL5418732 1 8.21
CHEMBL5397557 1 8.08
CHEMBL3813873 PEXIDARTINIB 4.0 1 8.01
CHEMBL5403510 1 7.92
CHEMBL5405639 1 7.82
CHEMBL5398307 1 7.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5432649 IC50 = 0.3 nM 9.52
CHEMBL5434318 IC50 = 0.3 nM 9.52
CHEMBL5417607 IC50 = 0.4 nM 9.40
CHEMBL5428404 IC50 = 0.5 nM 9.30
CHEMBL5406924 IC50 = 0.5 nM 9.30
CHEMBL5417494 IC50 = 0.7 nM 9.15
CHEMBL5406771 IC50 = 0.8 nM 9.10
CHEMBL5422465 IC50 = 0.8 nM 9.10
CHEMBL5431583 IC50 = 1.0 nM 9.00
CHEMBL5424694 IC50 = 1.0 nM 9.00
CHEMBL5403478 IC50 = 1.1 nM 8.96
CHEMBL5395449 IC50 = 1.2 nM 8.92
CHEMBL5411378 IC50 = 1.3 nM 8.89
CHEMBL5440766 IC50 = 1.7 nM 8.77
CHEMBL5439547 IC50 = 2.0 nM 8.70
CHEMBL5432592 IC50 = 2.1 nM 8.68
CHEMBL5414964 IC50 = 2.4 nM 8.62
CHEMBL5426924 IC50 = 2.5 nM 8.60
CHEMBL5406951 IC50 = 2.8 nM 8.55
CHEMBL5436096 IC50 = 2.8 nM 8.55
CHEMBL5417945 IC50 = 2.8 nM 8.55
CHEMBL5418474 IC50 = 3.7 nM 8.43
CHEMBL5438430 IC50 = 3.7 nM 8.43
CHEMBL5411522 IC50 = 5.2 nM 8.28
CHEMBL5418732 IC50 = 6.2 nM 8.21
CHEMBL5397557 IC50 = 8.3 nM 8.08
CHEMBL3813873 PEXIDARTINIB IC50 = 9.7 nM 8.01
CHEMBL5403510 IC50 = 12.0 nM 7.92
CHEMBL5405639 IC50 = 15.0 nM 7.82
CHEMBL5398307 IC50 = 55.0 nM 7.26
CHEMBL5419520 IC50 = 127.0 nM 6.90
CHEMBL5431339 IC50 = 180.0 nM 6.75
CHEMBL5398686 IC50 < 0.3 nM -
CHEMBL5404799 IC50 > 100.0 nM -