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Compound Detail

CHEMBL4448598

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O=C(COCCc1c[nH]nn1)N1Cc2cnc(NC3Cc4ccccc4C3)nc2C1

Basic Information

ChEMBL ID CHEMBL4448598
Phase Preclinical
Structure Type MOL
InChI Key ILOFWCAZDNILKY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

405.5
MW (Da)
1.28
ALogP
7
HBA
2
HBD
108.9
PSA (Ų)
0.57
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23N7O2
MW 405.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Autotaxin
CHEMBL3691
IC50 8.66 8.66 2.2 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1394.78 ng.hr.mL-1 Rattus norvegicus
Cmax 660.0 nM Rattus norvegicus
F 23.0 % Rattus norvegicus
T1/2 1.14 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Autotaxin IC50 = 2.2 nM 8.66 Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA lev... 27660691

Literature References

PubMed DOI Target Context # Activities
27660691 10.1021/acsmedchemlett.6b00207 ADMET 5
27660691 10.1021/acsmedchemlett.6b00207 Autotaxin 3
27660691 10.1021/acsmedchemlett.6b00207 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine