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Compound Detail

CHEMBL4875131

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CO[C@H]1CC[C@H](Nc2ncc(C(N)=O)c(NC34CC(C3)C4)n2)CC1

Basic Information

ChEMBL ID CHEMBL4875131
Phase Preclinical
Structure Type MOL
InChI Key QLEMSCWVMMVCEM-PHFHNXQFSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

331.4
MW (Da)
1.91
ALogP
6
HBA
3
HBD
102.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H25N5O2
MW 331.42
Aromatic Rings 1
Heavy Atoms 24
NP-Likeness -0.99

Activity Summary

IC50 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 8
CHEMBL2276
IC50 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2087.95 ng.hr.mL-1 Rattus norvegicus
CL 45.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34894681 10.1021/acs.jmedchem.1c01716 ADMET 6
34894681 10.1021/acs.jmedchem.1c01716 Mitogen-activated protein kinase 8 1

Data from ChEMBL 36 via Core Engine