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Compound Detail

CHEMBL82181

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Nc1nc(O)c2c(n1)NCC(CCc1cccc(C(=O)NC(CCC(=O)O)C(=O)O)c1)S2

Basic Information

ChEMBL ID CHEMBL82181
Phase Preclinical
Structure Type MOL
InChI Key KWZIRHHWDJUWDQ-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

461.5
MW (Da)
1.33
ALogP
9
HBA
6
HBD
187.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
9
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 2
Heavy Atoms 32
NP-Likeness -0.05

Activity Summary

IC50 3 meas. best 5.75
Ki 1 meas. best 8.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trifunctional purine biosynthetic protein adenosine-3
CHEMBL3972
Ki 8.47 8.47 3.4 1
CCRF-CEM
CHEMBL382
IC50 5.75 5.75 1800.0 1
L1210
CHEMBL386
IC50 5.55 5.095 2800.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9258357 10.1021/jm9607459 L1210 3
9258357 10.1021/jm9607459 Trifunctional purine biosynthetic protein adenosine-3 1
9258357 10.1021/jm9607459 CCRF-CEM 1
9258357 10.1021/jm9607459 Folylpolyglutamate synthase, mitochondrial 1
9258357 10.1021/jm9607459 Folate receptor alpha 1

Data from ChEMBL 36 via Core Engine