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Compound Detail

CHEMBL5189744

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CN1CCN(Cc2ccc(NC(=O)c3cccc(/N=N/c4cnc5ccccc5c4)c3)cc2C(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL5189744
Phase Preclinical
Structure Type MOL
InChI Key YNMSIILTLJXZKS-ULDVOPSXSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

532.6
MW (Da)
6.67
ALogP
6
HBA
1
HBD
73.2
PSA (Ų)
0.28
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27F3N6O
MW 532.57
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.62

Activity Summary

IC50 1 meas. best 8.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 8.02 8.02 9.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 208.0 hr -
T1/2 217.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35305461 10.1016/j.ejmech.2022.114226 No relevant target 2
35305461 10.1016/j.ejmech.2022.114226 Proto-oncogene tyrosine-protein kinase receptor Ret 1
35305461 10.1016/j.ejmech.2022.114226 ADMET 1

Data from ChEMBL 36 via Core Engine