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Compound Detail

CHEMBL4642409

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COc1ccc(-c2cnn3c(N)c(-c4ccccc4)c(OCCCN(C)C)nc23)cc1OC

Basic Information

ChEMBL ID CHEMBL4642409
Phase Preclinical
Structure Type MOL
InChI Key ATYKMHIJRBRZOA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
3.99
ALogP
8
HBA
1
HBD
87.1
PSA (Ų)
0.39
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N5O3
MW 447.54
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.93

Activity Summary

IC50 3 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET
CHEMBL3430888
IC50 7.16 7.16 70.0 1
LC-2-ad
CHEMBL2366260
IC50 5.55 5.55 2800.0 1
TEL/KDR
CHEMBL4630759
IC50 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32292564 10.1021/acsmedchemlett.0c00015 Kinesin-1 heavy chain/ Tyrosine-protein kinase receptor RET 1
32292564 10.1021/acsmedchemlett.0c00015 TEL/KDR 1
32292564 10.1021/acsmedchemlett.0c00015 LC-2-ad 1
32292564 10.1021/acsmedchemlett.0c00015 No relevant target 1

Data from ChEMBL 36 via Core Engine