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Compound Detail

CHEMBL4216289

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CN1CC[C@@](O)(C#Cc2cccc(-c3ccc(N)c(C(N)=O)n3)c2)C1=O

Basic Information

ChEMBL ID CHEMBL4216289
Phase Preclinical
Structure Type MOL
InChI Key LQQYQPONDYAXFT-IBGZPJMESA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

350.4
MW (Da)
0.37
ALogP
5
HBA
3
HBD
122.5
PSA (Ų)
0.68
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H18N4O3
MW 350.38
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.55

Activity Summary

IC50 1 meas. best 7.8
Ki 1 meas. best 10.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 14
CHEMBL5888
Ki 10.15 10.15 0.1 1
Mitogen-activated protein kinase kinase kinase 14
CHEMBL5888
IC50 7.8 7.8 16.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 5.6 mL.min-1.kg-1 Homo sapiens
CL 10.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29940120 10.1021/acs.jmedchem.8b00678 Mitogen-activated protein kinase kinase kinase 14 2
29940120 10.1021/acs.jmedchem.8b00678 ADMET 2
29940120 10.1021/acs.jmedchem.8b00678 No relevant target 1

Data from ChEMBL 36 via Core Engine