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Compound Detail

CHEMBL3660184

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N=C(N)c1ccc(CNC(=O)[C@H](CCC2CCNCC2)NC(=O)[C@@H](CCCc2cc[n+]([O-])cc2)NS(=O)(=O)Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL3660184
Phase Preclinical
Structure Type MOL
InChI Key BVZHCUOVJATBQP-IOWSJCHKSA-N
10
Targets
20
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

663.9
MW (Da)
2.00
ALogP
7
HBA
6
HBD
193.2
PSA (Ų)
0.06
QED
2
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H45N7O5S
MW 663.85
Aromatic Rings 3
Heavy Atoms 47
NP-Likeness -0.53

Activity Summary

Ki 20 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasminogen
CHEMBL1801
Ki 9.0 9.0 1.0 2
Plasma kallikrein
CHEMBL2000
Ki 8.4 8.4 4.0 2
Unchecked
CHEMBL612545
Ki 8.4 8.4 4.0 2
Coagulation factor X
CHEMBL244
Ki 6.4 6.4 400.0 2
Vitamin K-dependent protein C
CHEMBL4444
Ki 6.07 6.07 850.0 2
Coagulation factor XII
CHEMBL2821
Ki 6.06 6.06 870.0 2
Coagulation factor XI
CHEMBL2820
Ki 5.85 5.85 1400.0 2
Tissue-type plasminogen activator
CHEMBL1873
Ki 5.62 5.62 2400.0 2
Transcription initiation factor IIA subunit 1
CHEMBL4832
Ki 5.31 5.31 4900.0 2
Complement C1s subcomponent
CHEMBL3913
Ki 5.02 5.01 9500.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasminogen Ki = 1.0 nM 9.0 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Plasminogen Ki = 1.0 nM 9.0 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Plasma kallikrein Ki = 4.0 nM 8.4 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Plasma kallikrein Ki = 4.0 nM 8.4 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Unchecked Ki = 4.0 nM 8.4 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Unchecked Ki = 4.0 nM 8.4 Inhibition Assay: The inhibitory effect for the individual enzymes was determine... -
Coagulation factor X Ki = 400.0 nM 6.4 Inhibition Assay: Inhibition of human FXa was determined by the method described... -
Coagulation factor X Ki = 400.0 nM 6.4 Inhibition Assay: Inhibition of human FXa was determined by the method described... -
Vitamin K-dependent protein C Ki = 850.0 nM 6.07 Inhibition Assay: Inhibition of human aPC was determined by the method described... -
Vitamin K-dependent protein C Ki = 850.0 nM 6.07 Inhibition Assay: Inhibition of human aPC was determined by the method described... -
Coagulation factor XII Ki = 870.0 nM 6.06 Inhibition Assay: Inhibition of human alpha-FXIIa was determined by the method d... -
Coagulation factor XII Ki = 870.0 nM 6.06 Inhibition Assay: Inhibition of human alpha-FXIIa was determined by the method d... -
Coagulation factor XI Ki = 1400.0 nM 5.85 Inhibition Assay: Inhibition of human FXIa was determined by the method describe... -
Coagulation factor XI Ki = 1400.0 nM 5.85 Inhibition Assay: Inhibition of human FXIa was determined by the method describe... -
Tissue-type plasminogen activator Ki = 2400.0 nM 5.62 Inhibition Assay: Inhibition of human t-PA was determined by the method describe... -
Tissue-type plasminogen activator Ki = 2400.0 nM 5.62 Inhibition Assay: Inhibition of human t-PA was determined by the method describe... -
Transcription initiation factor IIA subunit 1 Ki = 4900.0 nM 5.31 Inhibition Assay: Inhibition of human FIIa was determined by the method describe... -
Transcription initiation factor IIA subunit 1 Ki = 4900.0 nM 5.31 Inhibition Assay: Inhibition of human FIIa was determined by the method describe... -
Complement C1s subcomponent Ki = 9500.0 nM 5.02 Inhibition Assay: Inhibition of human C1s was determined by the method described... -
Complement C1s subcomponent Ki = 10000.0 nM 5.0 Inhibition Assay: Inhibition of human C1s was determined by the method described... -

Data from ChEMBL 36 via Core Engine