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Compound Detail

CHEMBL1783852

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COc1ccc(CN2CCN(Cc3ccc(C(=O)N=C(N)N)cc3[N+](=O)[O-])CC2)c(OC)c1OC.Cl

Basic Information

ChEMBL ID CHEMBL1783852
Phase Preclinical
Structure Type MOL
InChI Key FRXRORZYYYSLKG-UHFFFAOYSA-N
Parent Compound CHEMBL1789669
Active Moiety CHEMBL1789669
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

486.5
MW (Da)
1.35
ALogP
8
HBA
2
HBD
158.8
PSA (Ų)
0.23
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H31ClN6O6
MW 522.99
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.96

Activity Summary

IC50 1 meas. best 8.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium/hydrogen exchanger 1
CHEMBL2577
IC50 8.44 8.44 3.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium/hydrogen exchanger 1 IC50 = 3.6 nM 8.44 Inhibition of NHE1-mediated rat platelet swelling 19433354

Literature References

PubMed DOI Target Context # Activities
19433354 10.1016/j.bmcl.2009.04.079 Rattus norvegicus 17
19433354 10.1016/j.bmcl.2009.04.079 Sodium/hydrogen exchanger 1 1

Data from ChEMBL 36 via Core Engine