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Compound Detail

CHEMBL114380

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COc1cnc(OCCOc2ncnc(NS(=O)(=O)c3ccc(C(C)(C)C)cc3)c2Oc2cccc(OC)c2)nc1

Basic Information

ChEMBL ID CHEMBL114380
Phase Preclinical
Structure Type MOL
InChI Key RTFQNQVCBCDGCX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

581.6
MW (Da)
4.63
ALogP
11
HBA
1
HBD
143.9
PSA (Ų)
0.23
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H31N5O7S
MW 581.65
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -1.11

Activity Summary

IC50 1 meas. best 10.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Endothelin-1 receptor
CHEMBL4130
IC50 10.82 10.82 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Endothelin-1 receptor IC50 = 0.015 nM 10.82 In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aor... 11585441

Literature References

PubMed DOI Target Context # Activities
11585441 10.1021/jm0102304 Endothelin-1 receptor 1

Data from ChEMBL 36 via Core Engine