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Compound Detail

CHEMBL5087283

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Cc1cc(Nc2cc(N3CCN(C)CC3)nc(Nc3ccc(CC(=O)Nc4ccc(C(C)C)cc4)cc3)n2)[nH]n1

Basic Information

ChEMBL ID CHEMBL5087283
Phase Preclinical
Structure Type MOL
InChI Key XTOAKVOIEPECCO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

539.7
MW (Da)
5.05
ALogP
8
HBA
4
HBD
114.1
PSA (Ų)
0.23
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H37N9O
MW 539.69
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.73

Activity Summary

IC50 1 meas. best 8.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 8.29 8.29 5.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35081714 10.1021/acs.jmedchem.1c01280 Proto-oncogene tyrosine-protein kinase receptor Ret 5
35081714 10.1021/acs.jmedchem.1c01280 Proto-oncogene tyrosine-protein kinase receptor Ret /Nuclear receptor coactivator 4 fusion protein 4
35081714 10.1021/acs.jmedchem.1c01280 Unchecked 2

Data from ChEMBL 36 via Core Engine