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Compound Detail

CHEMBL226714

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CN1CCN(C(=O)C2(NS(=O)(=O)c3ccc4c(Cl)cnc(N=C(N)N)c4c3)CCCC2)CC1

Basic Information

ChEMBL ID CHEMBL226714
Phase Preclinical
Structure Type MOL
InChI Key KHAPOCZPLRRWRN-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

494.0
MW (Da)
1.16
ALogP
6
HBA
3
HBD
147.0
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H28ClN7O3S
MW 494.02
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -1.19

Activity Summary

Ki 3 meas. best 8.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
Ki 8.85 8.85 1.4 1
Tissue-type plasminogen activator
CHEMBL1873
Ki 4.46 4.46 34700.0 1
Plasminogen
CHEMBL1801
Ki 4.19 4.19 65000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urokinase-type plasminogen activator Ki = 1.4 nM 8.85 Inhibition of human uPA 17447747
Tissue-type plasminogen activator Ki = 34700.0 nM 4.46 Inhibition of human tPA 17447747
Plasminogen Ki = 65000.0 nM 4.19 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