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Compound Detail

CHEMBL61257

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CCNC(=O)Nc1nc2nc(NCCCN3CCN(C)CC3)ncc2cc1-c1c(Cl)cccc1Cl

Basic Information

ChEMBL ID CHEMBL61257
Phase Preclinical
Structure Type MOL
InChI Key ZAPMLUQRTGRJST-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

517.5
MW (Da)
4.19
ALogP
7
HBA
3
HBD
98.3
PSA (Ų)
0.39
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30Cl2N8O
MW 517.47
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.46

Activity Summary

IC50 7 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proto-oncogene tyrosine-protein kinase Src
CHEMBL3655
IC50 7.62 7.62 24.0 1
Fibroblast growth factor receptor 1
CHEMBL3650
IC50 7.28 7.28 53.0 1
Platelet-derived growth factor receptor beta
CHEMBL2749
IC50 6.38 6.38 420.0 1
HT-29
CHEMBL384
IC50 6.05 6.05 900.0 1
SW-620
CHEMBL612262
IC50 5.6 5.6 2500.0 1
C6
CHEMBL614657
IC50 5.17 5.17 6700.0 1
HCT-8
CHEMBL613510
IC50 5.03 5.03 9300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11384237 10.1021/jm0004291 Platelet-derived growth factor receptor beta 1
11384237 10.1021/jm0004291 Fibroblast growth factor receptor 1 1
11384237 10.1021/jm0004291 Proto-oncogene tyrosine-protein kinase Src 1
11384237 10.1021/jm0004291 HCT-8 1
11384237 10.1021/jm0004291 SW-620 1
11384237 10.1021/jm0004291 HT-29 1
11384237 10.1021/jm0004291 C6 1

Data from ChEMBL 36 via Core Engine