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Compound Detail

CHEMBL5465171

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O=C1CCC(N2Cc3cc(C4CCN(C(=O)CCCCCN5CCC(c6ccc(Oc7nn8cnnc8c8c7CCCC8)cc6)CC5)CC4)ccc3C2=O)C(=O)N1

Basic Information

ChEMBL ID CHEMBL5465171
Phase Preclinical
Structure Type MOL
InChI Key HLNCBKSDCCIOPT-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

773.0
MW (Da)
5.70
ALogP
10
HBA
1
HBD
142.3
PSA (Ų)
0.15
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C44H52N8O5
MW 772.95
Aromatic Rings 4
Heavy Atoms 57
NP-Likeness -0.68

Activity Summary

IC50 3 meas. best 8.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methionine aminopeptidase 2
CHEMBL3922
IC50 8.24 8.08 5.8 2
Methionine aminopeptidase 2
CHEMBL1075272
IC50 8.23 8.23 5.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Methionine aminopeptidase 2 IC50 = 5.8 nM 8.24 METAP2 biochemical assay (human) -
Methionine aminopeptidase 2 IC50 = 5.9 nM 8.23 METAP2 biochemical assay (mouse) -
Methionine aminopeptidase 2 IC50 = 12.0 nM 7.92 2D HUVEC cells proliferation assay -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5463725 Methionine aminopeptidase 2 7
- 10.6019/CHEMBL5463725 D(2) dopamine receptor 2
- 10.6019/CHEMBL5463725 GABA-A receptor; anion channel 2
- 10.6019/CHEMBL5463725 Glutamate NMDA receptor 2
- 10.6019/CHEMBL5463725 Serine/threonine-protein kinase pim-2 1
- 10.6019/CHEMBL5463725 Beta-adrenergic receptor kinase 1 1
- 10.6019/CHEMBL5463725 Serine/threonine-protein kinase tousled-like 1 1
- 10.6019/CHEMBL5463725 TGF-beta receptor type-2 1
- 10.6019/CHEMBL5463725 Tyrosine-protein kinase HCK 1
- 10.6019/CHEMBL5463725 Dual specificity protein kinase CLK1 1
- 10.6019/CHEMBL5463725 Tyrosine-protein kinase Blk 1
- 10.6019/CHEMBL5463725 Tyrosine-protein kinase Lck 1
- 10.6019/CHEMBL5463725 Vasopressin V1a receptor 1
- 10.6019/CHEMBL5463725 Serine/threonine-protein kinase Sgk2 1
- 10.6019/CHEMBL5463725 eIF-2-alpha kinase GCN2 1
- 10.6019/CHEMBL5463725 Ribosomal protein S6 kinase alpha-5 1
- 10.6019/CHEMBL5463725 Megakaryocyte-associated tyrosine-protein kinase 1
- 10.6019/CHEMBL5463725 Tyrosine-protein kinase JAK2 1
- 10.6019/CHEMBL5463725 Hepatocyte growth factor receptor 1
- 10.6019/CHEMBL5463725 Tyrosine-protein kinase SYK 1

Data from ChEMBL 36 via Core Engine