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Compound Detail

CHEMBL4070056

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CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C(C)C)NC(=O)[C@@H]2CSCc3cc(cc(c3)CSC[C@@H](C(=O)N[C@@H](C)C(=O)N(C)CC(=O)N(C)CC(=O)N(C)CC(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCNC(=N)N)C(=O)O)NC1=O)CSC[C@H](NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4070056
Phase Preclinical
Structure Type MOL
InChI Key CUGMKURPXUMGSV-PHOGTTDVSA-N
13
Targets
15
Activities
1
Assay Types
1
PK Parameters
20
Publications
0
Known Names

Molecular Properties

2481.9
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C114H161N29O28S3
MW 2481.92

Activity Summary

Ki 15 meas. best 9.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasma kallikrein
CHEMBL2000
Ki 9.6 9.6 0.2 1
Unchecked
CHEMBL612545
Ki 9.07 7.4367 0.9 3
Plasma kallikrein
CHEMBL4105792
Ki 8.26 8.26 5.5 1
Plasma kallikrein
CHEMBL1250359
Ki 7.35 7.35 45.0 1
Kallikrein 1
CHEMBL4064
Ki 6.52 6.52 300.0 1
Coagulation factor XI
CHEMBL2820
Ki 6.3 6.3 500.0 1
Kallikrein-5
CHEMBL4447
Ki 6.1 6.1 800.0 1
Kallikrein-13
CHEMBL4863
Ki 6.09 6.09 820.0 1
Kallikrein-14
CHEMBL2641
Ki 5.7 5.7 2000.0 1
Kallikrein-2
CHEMBL2442
Ki 5.0 5.0 10000.0 1
Suppressor of tumorigenicity 14 protein
CHEMBL3018
Ki 4.82 4.82 15000.0 1
Coagulation factor X
CHEMBL244
Ki 4.64 4.64 23000.0 1
Kallikrein-1
CHEMBL2319
Ki 4.3 4.3 50000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 22.0 hr Oryctolagus cuniculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasma kallikrein Ki = 0.25 nM 9.6 Inhibition of human plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptid... 29517911
Unchecked Ki = 0.86 nM 9.07 Inhibition of cynomolgus monkey plasma kallikrein using fluorogenic H-Pro-Phe-Ar... 29517911
Plasma kallikrein Ki = 5.5 nM 8.26 Inhibition of recombinant Sprague-Dawley rat plasma kallikrein using fluorogenic... 29517911
Unchecked Ki = 22.0 nM 7.66 Inhibition of dog plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide ... 29517911
Plasma kallikrein Ki = 45.0 nM 7.35 Inhibition of recombinant mouse C-terminal 6His-tagged plasma kallikrein (20 to ... 29517911
Kallikrein 1 Ki = 300.0 nM 6.52 Inhibition of pig plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC peptide ... 29517911
Coagulation factor XI Ki = 500.0 nM 6.3 Inhibition of human factor 11a using fluorogenic peptide as substrate by fluores... 29517911
Kallikrein-5 Ki = 800.0 nM 6.1 Inhibition of recombinant human C-terminal 10His-tagged KLK5 (67 to 293 residues... 29517911
Kallikrein-13 Ki = 820.0 nM 6.09 Inhibition of recombinant human C-terminal polyHis-tagged KLK13 (1 to 262 residu... 29517911
Kallikrein-14 Ki = 2000.0 nM 5.7 Inhibition of recombinant human C-terminal 10His-tagged KLK14 (19 to 248 residue... 29517911
Unchecked Ki = 2650.0 nM 5.58 Inhibition of rabbit plasma kallikrein using fluorogenic H-Pro-Phe-Arg-AMC pepti... 29517911
Kallikrein-2 Ki = 10000.0 nM 5.0 Inhibition of recombinant human C-terminal 10His-tagged KLK2 (1 to 261 residues)... 29517911
Suppressor of tumorigenicity 14 protein Ki = 15000.0 nM 4.82 Inhibition of recombinant human N-terminal 6His-tagged matriptase catalytic doma... 29517911
Coagulation factor X Ki = 23000.0 nM 4.64 Inhibition of recombinant human C-terminal 10His-tagged factor Xa (24 to 488 res... 29517911
Kallikrein-1 Ki = 50000.0 nM 4.3 Inhibition of recombinant human C-terminal His-tagged KLK1 (1 to 262 residues) e... 29517911

Literature References

Data from ChEMBL 36 via Core Engine