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Compound Detail

CHEMBL4228960

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O=C(Nc1ccc2[nH]nc(-c3ccc(F)cc3)c2c1)C1CN(CC(=O)N2CC=C(c3ccc(-c4ncccn4)cc3)CC2)CCO1

Basic Information

ChEMBL ID CHEMBL4228960
Phase Preclinical
Structure Type MOL
InChI Key HMSWRYCPMVLGDS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

617.7
MW (Da)
4.78
ALogP
7
HBA
2
HBD
116.3
PSA (Ų)
0.27
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H32FN7O3
MW 617.69
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.77

Activity Summary

IC50 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 1
CHEMBL4040
IC50 6.92 6.92 119.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 1 IC50 = 119.0 nM 6.92 Inhibition of ERK2 (unknown origin) 29748051

Literature References

PubMed DOI Target Context # Activities
29748051 10.1016/j.bmcl.2018.04.063 Rattus norvegicus 1
29748051 10.1016/j.bmcl.2018.04.063 Mitogen-activated protein kinase 1 1

Data from ChEMBL 36 via Core Engine