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Compound Detail

CHEMBL3426431

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C=CCc1cc(F)cc(/C=N/NC(=O)CN2CCN(C(=O)c3ccc(C#N)cc3)CC2)c1O

Basic Information

ChEMBL ID CHEMBL3426431
Phase Preclinical
Structure Type MOL
InChI Key URHHGVGFSLCYIJ-JFLMPSFJSA-N
4
Targets
6
Activities
2
Assay Types
4
PK Parameters
9
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
2.04
ALogP
6
HBA
2
HBD
109.0
PSA (Ų)
0.38
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 C24H24FN5O3
MW 449.49
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.87

Activity Summary

IC50 5 meas. best 5.62
Kd 1 meas. best 8.86

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
No relevant target
CHEMBL2362975
Kd 8.86 8.86 1.4 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.62 5.2133 2400.0 3
Jurkat
CHEMBL397
IC50 5.46 5.46 3500.0 1
EL4
CHEMBL614293
IC50 5.29 5.29 5100.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6081.67 ng.hr.mL-1 Mus musculus
AUC 1753.33 ng.hr.mL-1 Mus musculus
F 28.8 % Mus musculus
T1/2 1.478 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine