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Compound Detail

CHEMBL214393

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O=c1ccn([C@@H]2O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]2O)c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL214393
Phase Preclinical
Structure Type MOL
InChI Key DJJCXFVJDGTHFX-XVFCMESISA-N
1
Targets
5
Activities
2
Assay Types
1
PK Parameters
10
Publications
0
Known Names

Molecular Properties

324.2
MW (Da)
-2.73
ALogP
8
HBA
5
HBD
171.3
PSA (Ų)
0.37
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C9H13N2O9P
MW 324.18
Aromatic Rings 1
Heavy Atoms 21
NP-Likeness 1.44

Activity Summary

Ki 4 meas.
Kd 1 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein argonaute-2
CHEMBL4680043
Kd 4.82 4.82 15000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 6.6 10^4/M Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein argonaute-2 Kd = 15000.0 nM 4.82 Binding affinity to human Argonaut protein 2 PAZ domain assessed as dissociation... 33132114

Literature References

PubMed DOI Target Context # Activities
33132114 10.1016/j.bmcl.2020.127637 Protein argonaute-2 4
17101674 10.1128/aac.00400-06 UMP-CMP kinase 3
17999967 10.1128/aac.01184-07 UMP-CMP kinase 3
16942026 10.1021/jm060485n P2Y purinoceptor 6 1
22991951 10.1021/jm301176r Orotidine phosphate decarboxylase 1
22991951 10.1021/jm301176r Uridine 5'-monophosphate synthase 1
22991951 10.1021/jm301176r Orotidine 5'-phosphate decarboxylase 1
23122937 10.1016/j.bmc.2012.09.067 Unchecked 1
29681152 10.1021/acs.jmedchem.7b01906 No relevant target 1
33488967 10.1021/acsmedchemlett.0c00440 Protein cereblon 1

Data from ChEMBL 36 via Core Engine