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Compound Detail

CHEMBL5437070

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[2H]C([2H])([2H])NC(=O)c1nnc(NC(=O)C2CC2)cc1Nc1cccc(-c2ncc(-c3cccnc3C(F)(F)F)cn2)c1OC

Basic Information

ChEMBL ID CHEMBL5437070
Phase Preclinical
Structure Type MOL
InChI Key UZWDRAZRBJVZNC-FIBGUPNXSA-N
Parent Compound CHEMBL5500142
Active Moiety CHEMBL5500142
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

564.5
MW (Da)
4.47
ALogP
9
HBA
3
HBD
143.9
PSA (Ų)
0.28
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23F3N8O3
MW 567.55
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.19

Activity Summary

IC50 1 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Signal transducer and activator of transcription 3
CHEMBL4026
IC50 8.62 8.62 2.4 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 22195.45 nM Mus musculus
T1/2 6.26 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36951608 10.1021/acs.jmedchem.2c01800 ADMET 3
36951608 10.1021/acs.jmedchem.2c01800 Signal transducer and activator of transcription 3 1

Data from ChEMBL 36 via Core Engine