CT-1578

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Synonyms
Status
Molecule Category UNKNOWN

Structure

InChI Key NNXDIGHYPZHXTR-ONEGZZNKSA-N
Smiles C1=C/COCc2cc(ccc2OCCN2CCCC2)Nc2nccc(n2)-c2ccc(o2)COC/1
InChI
InChI=1S/C26H30N4O4/c1-2-12-30(11-1)13-16-33-24-7-5-21-17-20(24)18-31-14-3-4-15-32-19-22-6-8-25(34-22)23-9-10-27-26(28-21)29-23/h3-10,17H,1-2,11-16,18-19H2,(H,27,28,29)/b4-3+

Bioactivity

Mechanism of Action Action Reference
Macrophage colony stimulating factor receptor inhibitor INHIBITOR PubMed
Protein: Tyrosine-protein kinase JAK2
Description: Tyrosine-protein kinase JAK2
Organism : Homo sapiens
O60674 ENSG00000096968
Protein: Macrophage colony stimulating factor receptor
Description: Macrophage colony-stimulating factor 1 receptor
Organism : Homo sapiens
P07333 ENSG00000182578
Protein: Tyrosine-protein kinase receptor FLT3
Description: Receptor-type tyrosine-protein kinase FLT3
Organism : Homo sapiens
P36888 ENSG00000122025
Assay Description Organism Bioactivity Reference
Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminometric assay None 46.0 nM
Inhibition of recombinant FLT3 using poly(Glu,Tyr) as substrate after 2 hrs by luminometric assay None 60.0 nM
Inhibition of TYK2 None 230.0 nM
Displacement of dofetilide from human ERG at 10 uM Homo sapiens 14.0 %
Inhibition of CDK9 None 36.0 nM
Inhibition of c-fms None 69.0 nM
Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutan Homo sapiens 0.246 nM
Antiarthritic activity in B10/R3 mouse immunized with bovine type2 collagen in Freund's complete adjuvant assessed as inhibition of increase in clinical arthritic scores at 105 mg/kg, po administered bid for 10 days measured for 10 days Mus musculus 23.0 %
Antiarthritic activity in B10/R3 mouse immunized with bovine type2 collagen in Freund's complete adjuvant assessed as inhibition of increase in clinical arthritic scores at 210 mg/kg, po administered bid for 10 days measured for 10 days Mus musculus 59.0 %
Inhibition of human CSF1R using poly[Glu:Tyr] (4:1) as substrate by [gamma-33P]-ATP assay Homo sapiens 69.0 nM

Cross References

Resources Reference
ChEMBL CHEMBL3544962
CONTENTS