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Compound Detail

CHEMBL3426725

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NCc1ccc(C(=O)Nc2ccncc2F)cc1-c1cccc(C(=O)Nc2ccc(CC(=O)OC3CCOCC3)cc2)c1

Basic Information

ChEMBL ID CHEMBL3426725
Phase Preclinical
Structure Type MOL
InChI Key BHTRISXBMWEIOP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

582.6
MW (Da)
5.12
ALogP
7
HBA
3
HBD
132.6
PSA (Ų)
0.23
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H31FN4O5
MW 582.63
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.81

Activity Summary

EC50 1 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
EC50 7.1 7.1 79.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1167 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 79.0 nM 7.1 Inhibition of ROCK-catalysed MLC Thr18/Ser19 phosphorylation in rat A7r5 cells a... 25898023

Literature References

PubMed DOI Target Context # Activities
25898023 10.1021/acs.jmedchem.5b00308 Plasma 3
25898023 10.1021/acs.jmedchem.5b00308 Rho-associated protein kinase 2 2
25898023 10.1021/acs.jmedchem.5b00308 Unchecked 1

Data from ChEMBL 36 via Core Engine