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Compound Detail

CHEMBL5569467

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Nc1nc2c(ncn2[C@H]2C[C@H](COCCP(=O)(O)O)N(C(=O)CCP(=O)(O)O)C2)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL5569467
Phase Preclinical
Structure Type MOL
InChI Key APDUDHYPFAMPGN-VHSXEESVSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

494.3
MW (Da)
-1.39
ALogP
9
HBA
6
HBD
234.2
PSA (Ų)
0.17
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H24N6O9P2
MW 494.34
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.10

Activity Summary

Ki 1 meas. best 6.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hypoxanthine-guanine phosphoribosyltransferase
CHEMBL2360
Ki 6.85 6.85 140.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hypoxanthine-guanine phosphoribosyltransferase Ki = 140.0 nM 6.85 Inhibition of human HGPRT by spectrophotometry 38651522

Literature References

PubMed DOI Target Context # Activities
38651522 10.1021/acs.jmedchem.4c00021 Unchecked 3
38651522 10.1021/acs.jmedchem.4c00021 Hypoxanthine-guanine phosphoribosyltransferase 2
38651522 10.1021/acs.jmedchem.4c00021 Hypoxanthine-guanine-xanthine phosphoribosyltransferase 1
38651522 10.1021/acs.jmedchem.4c00021 Xanthine-guanine phosphoribosyltransferase 1

Data from ChEMBL 36 via Core Engine