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Compound Detail

CHEMBL4752978

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CNC(=O)CN(Cc1ccccc1OC(F)F)C(=O)c1c[nH]c(C(=O)N2Cc3ccc(C(N)=O)cc3C2)n1

Basic Information

ChEMBL ID CHEMBL4752978
Phase Preclinical
Structure Type MOL
InChI Key JTCXCSWNNQIPRO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

526.5
MW (Da)
1.65
ALogP
6
HBA
3
HBD
150.7
PSA (Ų)
0.39
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24F2N6O5
MW 526.50
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.65

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
TAK1/TAB1
CHEMBL3038499
IC50 8.3 8.3 5.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
TAK1/TAB1 IC50 = 5.0 nM 8.3 Inhibition of recombinant human full-length His-tagged TAK1-TAB1 fusion protein ... 33859795

Literature References

PubMed DOI Target Context # Activities
33859795 10.1021/acsmedchemlett.0c00547 TAK1/TAB1 1
33859795 10.1021/acsmedchemlett.0c00547 Casein kinase II subunit alpha 1
33859795 10.1021/acsmedchemlett.0c00547 Casein kinase II subunit alpha' 1
33859795 10.1021/acsmedchemlett.0c00547 Receptor-type tyrosine-protein kinase FLT3 1
33859795 10.1021/acsmedchemlett.0c00547 Calcium-dependent protein kinase 1 1
33859795 10.1021/acsmedchemlett.0c00547 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 1
33859795 10.1021/acsmedchemlett.0c00547 Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma 1

Data from ChEMBL 36 via Core Engine