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Compound Detail

CHEMBL4211560

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CN1CC[C@@](O)(C#Cc2cccc(-c3cccc(C(N)=O)n3)c2)C1=O

Basic Information

ChEMBL ID CHEMBL4211560
Phase Preclinical
Structure Type MOL
InChI Key TZQDJUPUNBQRLX-IBGZPJMESA-N
1
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

335.4
MW (Da)
0.79
ALogP
4
HBA
2
HBD
96.5
PSA (Ų)
0.79
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 C19H17N3O3
MW 335.36
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.55

Activity Summary

IC50 1 meas. best 7.1
Ki 1 meas. best 9.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase kinase kinase 14
CHEMBL5888
Ki 9.38 9.38 0.4 1
Mitogen-activated protein kinase kinase kinase 14
CHEMBL5888
IC50 7.1 7.1 80.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.9 mL.min-1.kg-1 Homo sapiens
CL 7.1 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