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Compound Detail

CHEMBL2448400

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BP(=O)(OC[C@H]1O[C@@H](n2cnc3c(N)nc(SC)nc32)[C@H](O)[C@@H]1O)OP(=O)(O)CP(=O)(O)O

Basic Information

ChEMBL ID CHEMBL2448400
Phase Preclinical
Structure Type MOL
InChI Key ADRGMQYBPXHLCR-GHOYLPCTSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
14
Publications
0
Known Names

Molecular Properties

547.1
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H21BN5O11P3S
MW 547.13

Activity Summary

EC50 1 meas. best 4.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
P2Y purinoceptor 1
CHEMBL5720
EC50 4.76 4.76 17200.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 71.9 hr Homo sapiens
T1/2 14.5 hr -
T1/2 14.5 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
P2Y purinoceptor 1 EC50 = 17200.0 nM 4.76 Agonist activity at turkey P2Y1 receptor expressed in human 1321N1 cells assesse... 18760862

Literature References

PubMed DOI Target Context # Activities
18760862 10.1016/j.ejmech.2008.07.015 P2Y purinoceptor 6 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleoside triphosphate diphosphohydrolase 1 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleoside triphosphate diphosphohydrolase 2 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleoside triphosphate diphosphohydrolase 3 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleoside triphosphate diphosphohydrolase 8 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 4
18760862 10.1016/j.ejmech.2008.07.015 Ectonucleotide pyrophosphatase/phosphodiesterase family member 3 4
18760862 10.1016/j.ejmech.2008.07.015 P2Y purinoceptor 1 4
18760862 10.1016/j.ejmech.2008.07.015 P2Y purinoceptor 2 4
18760862 10.1016/j.ejmech.2008.07.015 P2Y purinoceptor 4 4
20337495 10.1021/jm100030u No relevant target 3
18760862 10.1016/j.ejmech.2008.07.015 Serum 2
18760862 10.1016/j.ejmech.2008.07.015 ADMET 2
18760862 10.1016/j.ejmech.2008.07.015 No relevant target 1

Data from ChEMBL 36 via Core Engine