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Compound Detail

CHEMBL227607

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CN(C)CCN(C1(C(=O)O)CCCC1)S(=O)(=O)c1ccc2c(Cl)cnc(N=C(N)N)c2c1

Basic Information

ChEMBL ID CHEMBL227607
Phase Preclinical
Structure Type MOL
InChI Key LIPQMUVUZWSFOR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

483.0
MW (Da)
1.74
ALogP
6
HBA
3
HBD
155.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H27ClN6O4S
MW 482.99
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.72

Activity Summary

Ki 3 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
Ki 8.59 8.59 2.6 1
Tissue-type plasminogen activator
CHEMBL1873
Ki 4.64 4.64 23000.0 1
Plasminogen
CHEMBL1801
Ki 4.5 4.5 32000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urokinase-type plasminogen activator Ki = 2.6 nM 8.59 Inhibition of human uPA 17447747
Tissue-type plasminogen activator Ki = 23000.0 nM 4.64 Inhibition of human tPA 17447747
Plasminogen Ki = 32000.0 nM 4.5 Inhibition of human plasmin 17447747

Literature References

PubMed DOI Target Context # Activities
17447747 10.1021/jm061066t Urokinase-type plasminogen activator 1
17447747 10.1021/jm061066t Tissue-type plasminogen activator 1
17447747 10.1021/jm061066t Plasminogen 1

Data from ChEMBL 36 via Core Engine