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Compound Detail

CHEMBL4643936

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O=C1CCC(N2C(=O)c3ccc(N4CC(C(=O)N5CCN(c6cccc(-c7cnc8ccc(N9CCC[C@@H]9c9cccc(F)c9)nn78)n6)CC5)C4)cc3C2=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL4643936
Phase Preclinical
Structure Type MOL
InChI Key KBDADBOMDMRDQP-KWRHIPAJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

782.8
MW (Da)
3.46
ALogP
12
HBA
1
HBD
156.7
PSA (Ų)
0.24
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H39FN10O5
MW 782.84
Aromatic Rings 5
Heavy Atoms 58
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KM12
CHEMBL614709
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KM12 IC50 = 2.0 nM 8.7 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