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Compound Detail

CHEMBL4649362

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O=C1CCC(N2C(=O)c3cccc(NCCCC(=O)N4CCN(c5ccc(C(=O)Nc6n[nH]c7ccc(Cc8cc(F)cc(F)c8)cc67)c(NC6CCOCC6)c5)CC4)c3C2=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL4649362
Phase Preclinical
Structure Type MOL
InChI Key XIQKGMBOWICGJW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

887.9
MW (Da)
5.22
ALogP
11
HBA
5
HBD
198.2
PSA (Ų)
0.08
QED
3
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C47H47F2N9O7
MW 887.94
Aromatic Rings 5
Heavy Atoms 65
NP-Likeness -1.10

Activity Summary

IC50 1 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KM12
CHEMBL614709
IC50 8.82 8.82 1.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KM12 IC50 = 1.5 nM 8.82 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