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Compound Detail

CHEMBL1779516

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O=C1NCC2(CCCC2)c2[nH]c(-c3ccnc(-c4cnc5ccccc5c4)n3)cc21

Basic Information

ChEMBL ID CHEMBL1779516
Phase Preclinical
Structure Type MOL
InChI Key QQKYFJMFTLSOKW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

395.5
MW (Da)
4.24
ALogP
4
HBA
2
HBD
83.6
PSA (Ų)
0.53
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 C24H21N5O
MW 395.47
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.55

Activity Summary

EC50 1 meas. best 6.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-activated protein kinase 2
CHEMBL2208
EC50 6.63 6.63 234.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21565500 10.1016/j.bmcl.2011.04.018 ADMET 2
21565500 10.1016/j.bmcl.2011.04.018 Liver microsomes 2
21565500 10.1016/j.bmcl.2011.04.018 MAP kinase-activated protein kinase 2 1
21565500 10.1016/j.bmcl.2011.04.018 Caco-2 1
21565500 10.1016/j.bmcl.2011.04.018 No relevant target 1
21565500 10.1016/j.bmcl.2011.04.018 THP-1 1

Data from ChEMBL 36 via Core Engine