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Compound Detail

CHEMBL2158678

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Nc1nc2[nH]c(CCCCc3sccc3C(=O)N[C@@H](CCC(=O)O)C(=O)O)cc2c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL2158678
Phase Preclinical
Structure Type MOL
InChI Key KPLUEWVRYVJTJJ-ZDUSSCGKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

461.5
MW (Da)
1.51
ALogP
7
HBA
6
HBD
191.3
PSA (Ų)
0.23
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H23N5O6S
MW 461.50
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.27

Activity Summary

IC50 1 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KB
CHEMBL398
IC50 6.77 6.77 171.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KB IC50 = 171.0 nM 6.77 Growth inhibition of human KB cells endogenously expressing RFC/FRalpha/PCFT inc... 22243528

Literature References

PubMed DOI Target Context # Activities
22243528 10.1021/jm201688n R2 3
22243528 10.1021/jm201688n NON-PROTEIN TARGET 3
22243528 10.1021/jm201688n IGROV-1 2
22243528 10.1021/jm201688n KB 2
22243528 10.1021/jm201688n Folate receptor alpha 1

Data from ChEMBL 36 via Core Engine