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Compound Detail

CHEMBL3955549

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CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(N)=O)C(C)C)C(C)C

Basic Information

ChEMBL ID CHEMBL3955549
Phase Preclinical
Structure Type BOTH
InChI Key ONNGEGKKEUTKEN-RWZNXTNUSA-N
2
Targets
15
Activities
3
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

2486.9
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C116H180N32O29
MW 2486.91

Activity Summary

EC50 9 meas. best 6.07
IC50 5 meas. best 7.07
Kd 1 meas. best 7.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 7.47 7.47 33.8 1
Tissue factor pathway inhibitor
CHEMBL3713062
IC50 7.07 7.01 85.0 5
Tissue factor pathway inhibitor
CHEMBL3713062
EC50 6.07 5.7256 850.0 9

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked Kd = 33.8 nM 7.47 Binding affinity to C-terminal 10x-His-tagged human TFPI-1 (29 to 282 residues) ... -
Tissue factor pathway inhibitor IC50 = 85.0 nM 7.07 Binding affinity to immobilized human TFPI-1alpha assessed as inhibition of biot... -
Tissue factor pathway inhibitor IC50 = 85.0 nM 7.07 Binding affinity to TFPI (unknown origin) incubated for 1.5 hrs using tracer pep... -
Tissue factor pathway inhibitor IC50 = 85.0 nM 7.07 Binding affinity to TFPI (unknown origin) incubated for 1.5 hrs using tracer pep... -
Tissue factor pathway inhibitor IC50 = 119.0 nM 6.92 Binding affinity to TFPI (unknown origin) incubated for 1.5 hrs using tracer pep... -
Tissue factor pathway inhibitor IC50 = 119.0 nM 6.92 Binding affinity to TFPI (unknown origin) incubated for 1.5 hrs using tracer pep... -
Tissue factor pathway inhibitor EC50 = 850.0 nM 6.07 Inhibition of TFPI in FVIII inhibited human plasma assessed as reduction in thro... -
Tissue factor pathway inhibitor EC50 = 850.0 nM 6.07 Inhibition of TFPI in human plasma with induced factor-8 deficiency assessed as ... -
Tissue factor pathway inhibitor EC50 = 850.0 nM 6.07 Inhibition of TFPI in human plasma with induced factor-8 deficiency assessed as ... -
Tissue factor pathway inhibitor EC50 = 880.0 nM 6.06 Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assesse... -
Tissue factor pathway inhibitor EC50 = 920.0 nM 6.04 Inhibition of TFPI (unknown origin) using FXa-specific chromogenic substrate S22... -
Tissue factor pathway inhibitor EC50 = 920.0 nM 6.04 Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assesse... -
Tissue factor pathway inhibitor EC50 = 8800.0 nM 5.06 Inhibition of TFPI (unknown origin) using FXa-specific chromogenic substrate S22... -
Tissue factor pathway inhibitor EC50 = 8800.0 nM 5.06 Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assesse... -
Tissue factor pathway inhibitor EC50 = 8800.0 nM 5.06 Inhibition of C-terminus 10x-His-taged human TFPI-1 (29 to 282 residues) assesse... -

Data from ChEMBL 36 via Core Engine