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Assay Detail

CHEMBL4728940

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

Binding
Inhibition of CSF1R in mouse NFS-60 cells assessed as reduction in CSF-induced cell proliferation after 72 hrs by CellTiter-Glo assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type NFS-60
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Macrophage colony-stimulating factor 1 receptor (CHEMBL5570)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of IACS-9439, a Potent, Exquisitely Selective, and Orally Bioavailable Inhibitor of CSF1R.
Czako B,Marszalek JR,Burke JP,Mandal P,Leonard PG,Cross JB,Mseeh F,Jiang Y,Chang EQ,Suzuki E,Kovacs JJ,Feng N,Gera S,Harris AL,Liu Z,Mullinax RA,Pang J,Parker CA,Spencer ND,Yu SS,Wu Q,Tremblay MR,Mikule K,Wilcoxen K,Heffernan TP,Draetta GF,Jones P
J Med Chem (2020) 63 : 9888 -9911
PubMed 32787110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.78 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4758092 1 8.15
CHEMBL4748740 1 8.15
CHEMBL4740157 1 7.85
CHEMBL4779197 1 7.58
CHEMBL4763289 1 7.32
CHEMBL4741283 1 7.30
CHEMBL4779878 1 7.22
CHEMBL4754431 1 7.09
CHEMBL4798876 1 7.01
CHEMBL4787609 1 6.98
CHEMBL4798601 1 6.98
CHEMBL4763875 1 6.90
CHEMBL4759047 1 6.88
CHEMBL4762843 1 6.75
CHEMBL4756510 1 6.72
CHEMBL4795462 1 6.71
CHEMBL4788945 1 6.64
CHEMBL4790139 1 6.57
CHEMBL4751287 1 6.54
CHEMBL4746711 1 6.46
CHEMBL4788832 1 6.30
CHEMBL4798920 1 6.03
CHEMBL4764974 1 5.92
CHEMBL4743008 1 5.88
CHEMBL4751359 1 5.84
CHEMBL4777344 1 5.64
CHEMBL4783368 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4758092 IC50 = 7.0 nM 8.15
CHEMBL4748740 IC50 = 7.0 nM 8.15
CHEMBL4740157 IC50 = 14.0 nM 7.85
CHEMBL4779197 IC50 = 26.0 nM 7.58
CHEMBL4763289 IC50 = 48.0 nM 7.32
CHEMBL4741283 IC50 = 50.0 nM 7.30
CHEMBL4779878 IC50 = 60.0 nM 7.22
CHEMBL4754431 IC50 = 82.0 nM 7.09
CHEMBL4798876 IC50 = 98.0 nM 7.01
CHEMBL4787609 IC50 = 105.0 nM 6.98
CHEMBL4798601 IC50 = 104.0 nM 6.98
CHEMBL4763875 IC50 = 125.0 nM 6.90
CHEMBL4759047 IC50 = 133.0 nM 6.88
CHEMBL4762843 IC50 = 178.0 nM 6.75
CHEMBL4756510 IC50 = 189.0 nM 6.72
CHEMBL4795462 IC50 = 194.0 nM 6.71
CHEMBL4788945 IC50 = 228.0 nM 6.64
CHEMBL4790139 IC50 = 270.0 nM 6.57
CHEMBL4751287 IC50 = 288.0 nM 6.54
CHEMBL4746711 IC50 = 345.0 nM 6.46
CHEMBL4788832 IC50 = 504.0 nM 6.30
CHEMBL4798920 IC50 = 930.0 nM 6.03
CHEMBL4764974 IC50 = 1204.0 nM 5.92
CHEMBL4743008 IC50 = 1304.0 nM 5.88
CHEMBL4751359 IC50 = 1455.0 nM 5.84
CHEMBL4777344 IC50 = 2269.0 nM 5.64
CHEMBL4783368 IC50 = 2511.0 nM 5.60