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Compound Detail

CHEMBL2165617

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O=C(O)Cn1ccc(NC(=O)[C@H](CC2CCCC2)n2cnc(C(F)(F)F)c2)n1

Basic Information

ChEMBL ID CHEMBL2165617
Phase Preclinical
Structure Type MOL
InChI Key HHSZUJCBROAKTA-LBPRGKRZSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

399.4
MW (Da)
2.94
ALogP
6
HBA
2
HBD
102.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H20F3N5O3
MW 399.37
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -1.31

Activity Summary

EC50 1 meas. best 5.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 5.97 5.97 1080.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 8.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 1080.0 nM 5.97 Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophoto... 22196621

Literature References

PubMed DOI Target Context # Activities
22196621 10.1021/jm2014887 Hexokinase-4 2
22196621 10.1021/jm2014887 ADMET 1
22196621 10.1021/jm2014887 Liver microsomes 1
22196621 10.1021/jm2014887 Solute carrier organic anion transporter family member 1B3 1

Data from ChEMBL 36 via Core Engine