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Compound Detail

CHEMBL3355156

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Cc1ccc(NC(=O)c2ccc(F)c(-n3cc(NC(=O)Nc4ccccc4Cl)cn3)c2)cn1

Basic Information

ChEMBL ID CHEMBL3355156
Phase Preclinical
Structure Type MOL
InChI Key JVSLZGKNRZILCQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
12
Publications
0
Known Names

Molecular Properties

464.9
MW (Da)
5.26
ALogP
5
HBA
3
HBD
100.9
PSA (Ų)
0.37
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18ClFN6O2
MW 464.89
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -2.50

Activity Summary

IC50 3 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 10
CHEMBL2637
IC50 7.1 7.1 80.0 1
Mitogen-activated protein kinase 9
CHEMBL4179
IC50 6.83 6.83 148.0 1
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 5.62 5.62 2369.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.8333 hr Homo sapiens
T1/2 1.433 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25393557 10.1021/jm501256y No relevant target 2
25393557 10.1021/jm501256y Mitogen-activated protein kinase 10 1
25393557 10.1021/jm501256y Mitogen-activated protein kinase 8 1
25393557 10.1021/jm501256y Unchecked 1
25393557 10.1021/jm501256y Mitogen-activated protein kinase 9 1
25393557 10.1021/jm501256y Mitogen-activated protein kinase 14 1
25393557 10.1021/jm501256y Liver microsome 1
25393557 10.1021/jm501256y Liver 1
25393557 10.1021/jm501256y Cytochrome P450 1A2 1
25393557 10.1021/jm501256y Cytochrome P450 2C9 1
25393557 10.1021/jm501256y Cytochrome P450 2D6 1
25393557 10.1021/jm501256y Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine