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Compound Detail

CHEMBL3426429

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C=CCc1cc(F)cc(/C=N/NC(=O)CN2CCN(C(=O)c3ccccc3)CC2)c1O

Basic Information

ChEMBL ID CHEMBL3426429
Phase Preclinical
Structure Type MOL
InChI Key RTEMYTVPGXXMRH-MFKUBSTISA-N
4
Targets
6
Activities
2
Assay Types
4
PK Parameters
9
Publications
0
Known Names

Molecular Properties

424.5
MW (Da)
2.17
ALogP
5
HBA
2
HBD
85.2
PSA (Ų)
0.41
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 C23H25FN4O3
MW 424.48
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.67

Activity Summary

IC50 5 meas. best 5.47
Kd 1 meas. best 8.97

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
No relevant target
CHEMBL2362975
Kd 8.97 8.97 1.1 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.47 5.18 3400.0 3
Jurkat
CHEMBL397
IC50 5.39 5.39 4100.0 1
EL4
CHEMBL614293
IC50 5.14 5.14 7300.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 4850.0 ng.hr.mL-1 Mus musculus
AUC 428.33 ng.hr.mL-1 Mus musculus
F 8.5 % Mus musculus
T1/2 2.008 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

Data from ChEMBL 36 via Core Engine