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Compound Detail

CHEMBL5076509

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Cn1cnc2ncn(Cc3nc([C@@H]4CO[C@@H](c5ccc(F)cc5)C4)no3)c(=O)c21

Basic Information

ChEMBL ID CHEMBL5076509
Phase Preclinical
Structure Type MOL
InChI Key KVSPYEYQFMGJNK-GXTWGEPZSA-N
3
Targets
6
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

396.4
MW (Da)
1.95
ALogP
9
HBA
0
HBD
100.9
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H17FN6O3
MW 396.38
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.26

Activity Summary

IC50 6 meas. best 8.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily A member 1
CHEMBL6007
IC50 8.25 7.965 5.6 4
Transient receptor potential cation channel subfamily A member 1
CHEMBL5160
IC50 8.15 8.15 7.0 1
Unchecked
CHEMBL612545
IC50 8.12 8.12 7.6 1

Pharmacokinetic Data

Parameter Value Units Species
CL 4.3 mL.min-1.kg-1 Homo sapiens
CL 9.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33749283 10.1021/acs.jmedchem.0c02023 ADMET 2
33749283 10.1021/acs.jmedchem.0c02023 Unchecked 1
33749283 10.1021/acs.jmedchem.0c02023 No relevant target 1
37269667 10.1016/j.ejmech.2023.115392 Transient receptor potential cation channel subfamily A member 1 1

Data from ChEMBL 36 via Core Engine