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Compound Detail

CHEMBL5185302

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CN1CCN(Cc2ccc(NC(=O)c3ccc(F)c(/N=N\c4cnc5ccccc5c4)c3F)cc2C(F)(F)F)CC1

Basic Information

ChEMBL ID CHEMBL5185302
Phase Preclinical
Structure Type MOL
InChI Key URVIRFMFFZIHOH-DTTHWBISSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

568.5
MW (Da)
6.95
ALogP
6
HBA
1
HBD
73.2
PSA (Ų)
0.20
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25F5N6O
MW 568.55
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.62

Activity Summary

IC50 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 7.77 7.77 17.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 38.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine