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Compound Detail

CHEMBL5094196

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CCN1CCN(c2cc(Nc3cc(C)n[nH]3)nc(Nc3ccc(CC(=O)NCc4cccc(F)c4)cc3)n2)CC1

Basic Information

ChEMBL ID CHEMBL5094196
Phase Preclinical
Structure Type MOL
InChI Key GOUCBHDPFPFCLN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

543.6
MW (Da)
4.14
ALogP
8
HBA
4
HBD
114.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H34FN9O
MW 543.65
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -2.11

Activity Summary

IC50 1 meas. best 7.91

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 7.91 7.91 12.4 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