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Compound Detail

CHEMBL4639369

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O=C1CCC(N2C(=O)c3ccc(NCCCCC(=O)N4CCN(c5cccc(-c6cnc7ccc(N8CCC[C@@H]8c8cccc(F)c8)nn67)n5)CC4)cc3C2=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL4639369
Phase Preclinical
Structure Type MOL
InChI Key ATSQWPUJIXUSHQ-BONSOQDYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

798.9
MW (Da)
4.60
ALogP
12
HBA
2
HBD
165.4
PSA (Ų)
0.14
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H43FN10O5
MW 798.88
Aromatic Rings 5
Heavy Atoms 59
NP-Likeness -1.34

Activity Summary

IC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KM12
CHEMBL614709
IC50 9.05 9.05 0.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KM12 IC50 = 0.9 nM 9.05 Antiproliferative activity against human KM12 cells expressing TPM3-TRKA assesse... 32550985

Literature References

PubMed DOI Target Context # Activities
32550985 10.1021/acsmedchemlett.0c00235 KM12 1

Data from ChEMBL 36 via Core Engine