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Compound Detail

CHEMBL1783748

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Cc1ccc(NC(=O)[C@H](CC2CCC(F)(F)CC2)n2ccc(S(=O)(=O)C(C)C)cc2=O)nc1

Basic Information

ChEMBL ID CHEMBL1783748
Phase Preclinical
Structure Type MOL
InChI Key CKPHRGNLPYRZKJ-IBGZPJMESA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
2
Publications
0
Known Names

Molecular Properties

481.6
MW (Da)
4.13
ALogP
6
HBA
1
HBD
98.1
PSA (Ų)
0.64
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 C23H29F2N3O4S
MW 481.57
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.06

Activity Summary

EC50 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hexokinase-4
CHEMBL3820
EC50 6.8 6.8 160.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 36.0 mL.min-1.kg-1 Rattus norvegicus
CL 8.0 mL.min-1.kg-1 Homo sapiens
T1/2 0.7 hr Rattus norvegicus
T1/2 1.217 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hexokinase-4 EC50 = 160.0 nM 6.8 Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophoto... 19435665

Literature References

PubMed DOI Target Context # Activities
19435665 10.1016/j.bmcl.2009.04.107 Liver microsomes 4
19435665 10.1016/j.bmcl.2009.04.107 Hexokinase-4 2

Data from ChEMBL 36 via Core Engine