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Compound Detail

CHEMBL4227512

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CC[C@@]1(C(=O)Nc2ccc3[nH]nc(-c4ccc(F)cc4)c3c2)CCN(CC(=O)N2CC=C(c3ccc(-c4ncccn4)cc3)CC2)C1

Basic Information

ChEMBL ID CHEMBL4227512
Phase Preclinical
Structure Type MOL
InChI Key BDYNWNOOTJXZLX-DIPNUNPCSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

629.7
MW (Da)
6.18
ALogP
6
HBA
2
HBD
107.1
PSA (Ų)
0.21
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H36FN7O2
MW 629.74
Aromatic Rings 5
Heavy Atoms 47
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 6.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 1
CHEMBL4040
IC50 6.94 6.94 115.0 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 = 115.0 nM 6.94 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