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Compound Detail

CHEMBL5803781

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COC(=O)/C=C/CC[C@H](NC(=O)c1ccncc1C(=O)O)C(=O)N[C@H](C(=O)N1CC(=O)C[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(N)=O)C1CCCCC1)C1CCCCC1)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL5803781
Phase Preclinical
Structure Type MOL
InChI Key NPPFXOSTKHCNFF-XLZLINMASA-N
7
Targets
24
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

838.0
MW (Da)
1.70
ALogP
11
HBA
6
HBD
273.4
PSA (Ų)
0.10
QED
3
Ro5 Violations
17
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C42H59N7O11
MW 837.97
Aromatic Rings 1
Heavy Atoms 60
NP-Likeness 0.19

Activity Summary

IC50 24 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XIII A/B chain
CHEMBL6066544
IC50 8.4 8.2 4.0 2
Unchecked
CHEMBL612545
IC50 8.15 7.4523 7.0 13
Coagulation factor XIII A chain
CHEMBL4530
IC50 7.8 7.71 16.0 4
Protein-glutamine gamma-glutamyltransferase 6
CHEMBL2079852
IC50 7.77 7.77 17.0 1
Protein-glutamine gamma-glutamyltransferase
CHEMBL2730
IC50 7.17 6.76 67.0 2
Protein-glutamine gamma-glutamyltransferase K
CHEMBL2810
IC50 4.96 4.96 11035.0 1
Protein-glutamine gamma-glutamyltransferase E
CHEMBL3363
IC50 4.18 4.18 66511.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XIII A/B chain IC50 = 4.0 nM 8.4 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 7.0 nM 8.15 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 8.0 nM 8.1 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Coagulation factor XIII A/B chain IC50 = 10.0 nM 8.0 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 15.0 nM 7.82 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 15.0 nM 7.82 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Coagulation factor XIII A chain IC50 = 16.0 nM 7.8 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 16.0 nM 7.8 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Coagulation factor XIII A chain IC50 = 16.0 nM 7.8 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 17.0 nM 7.77 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Protein-glutamine gamma-glutamyltransferase 6 IC50 = 17.0 nM 7.77 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 19.0 nM 7.72 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 19.0 nM 7.72 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 20.0 nM 7.7 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Coagulation factor XIII A chain IC50 = 24.0 nM 7.62 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 24.0 nM 7.62 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Coagulation factor XIII A chain IC50 = 24.0 nM 7.62 Transamidation Assay for Determining Inhibitor Selectivity: The most relevant of... -
Unchecked IC50 = 28.0 nM 7.55 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Protein-glutamine gamma-glutamyltransferase IC50 = 67.0 nM 7.17 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -
Unchecked IC50 = 365.0 nM 6.44 Isopeptidase Assay for Estimating Inhibitor Potency: FXIIIa activity has been de... -

Data from ChEMBL 36 via Core Engine