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Compound Detail

CHEMBL4205942

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Cc1ccc(Nc2ncc3c(n2)N(C)C(=O)N(c2cc(NC(=O)c4cc(N5CCC(O)CC5)cc(C(F)(F)F)c4)ccc2C)C3)cn1

Basic Information

ChEMBL ID CHEMBL4205942
Phase Preclinical
Structure Type MOL
InChI Key PIMBZWQACDWQJV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

646.7
MW (Da)
6.04
ALogP
8
HBA
3
HBD
126.8
PSA (Ų)
0.23
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H33F3N8O3
MW 646.67
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -1.51

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Activated CDC42 kinase 1
CHEMBL4599
IC50 7.4 7.4 40.0 1
Mitogen-activated protein kinase kinase kinase kinase 2
CHEMBL5330
IC50 7.14 7.14 72.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30153003 10.1021/acs.jmedchem.8b00882 OCI-AML-3 2
30153003 10.1021/acs.jmedchem.8b00882 Activated CDC42 kinase 1 1
30153003 10.1021/acs.jmedchem.8b00882 Mitogen-activated protein kinase kinase kinase kinase 2 1
30153003 10.1021/acs.jmedchem.8b00882 BaF3 1
30153003 10.1021/acs.jmedchem.8b00882 Unchecked 1
30153003 10.1021/acs.jmedchem.8b00882 U-937 1

Data from ChEMBL 36 via Core Engine