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Compound Detail

CHEMBL3735992

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C[C@H](CCC(=O)N[C@H](CC(=O)O)Cc1c[nH]c2ccccc12)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C

Basic Information

ChEMBL ID CHEMBL3735992
Phase Preclinical
Structure Type MOL
InChI Key DYQSTAGJKVMDAE-LWIYDJPKSA-N
12
Targets
13
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

574.8
MW (Da)
7.03
ALogP
3
HBA
4
HBD
102.4
PSA (Ų)
0.24
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H50N2O4
MW 574.81
Aromatic Rings 2
Heavy Atoms 42
NP-Likeness 1.56

Activity Summary

IC50 12 meas. best 5.75
Ki 1 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ephrin type-A receptor 2
CHEMBL4105859
Ki 5.85 5.85 1400.0 1
Ephrin type-A receptor 8
CHEMBL4739670
IC50 5.75 5.75 1800.0 1
Ephrin type-A receptor 1
CHEMBL5810
IC50 5.66 5.66 2200.0 1
Ephrin type-A receptor 4
CHEMBL1293259
IC50 5.55 5.55 2800.0 1
Ephrin type-A receptor 6
CHEMBL4739690
IC50 5.54 5.54 2900.0 1
Ephrin type-A receptor 5
CHEMBL4739679
IC50 5.52 5.52 3000.0 1
Ephrin type-A receptor 3
CHEMBL2034794
IC50 5.39 5.39 4100.0 1
Ephrin type-A receptor 2
CHEMBL2068
IC50 5.37 5.37 4265.8 1
Ephrin type-A receptor 7
CHEMBL4739689
IC50 5.35 5.35 4500.0 1
Ephrin type-A receptor 2
CHEMBL4105859
IC50 5.27 5.27 5400.0 1
Ephrin type-B receptor 1
CHEMBL4739675
IC50 5.11 5.11 7700.0 1
Ephrin type-B receptor 3
CHEMBL4739678
IC50 5.01 5.01 9800.0 1
Ephrin type-B receptor 2
CHEMBL5961
IC50 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Ephrin type-A receptor 2 Ki = 1400.0 nM 5.85 Displacement of biotinylated Fc-tagged ephrin-A1 from C/N-terminal 6-His tag mou... 39024966
Ephrin type-A receptor 8 IC50 = 1800.0 nM 5.75 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 1 IC50 = 2200.0 nM 5.66 Displacement of biotinylated Fc-tagged ephrin-A1 from N/C-terminal 6-his tagged ... 39024966
Ephrin type-A receptor 4 IC50 = 2800.0 nM 5.55 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 6 IC50 = 2900.0 nM 5.54 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 5 IC50 = 3000.0 nM 5.52 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 3 IC50 = 4100.0 nM 5.39 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 2 IC50 = 4265.8 nM 5.37 Displacement of biotinylated-ephrin-A1-Fc from EphA2-Fc receptor (unknown origin... 26363867
Ephrin type-A receptor 7 IC50 = 4500.0 nM 5.35 Displacement of biotinylated Fc-tagged ephrin-A1 from recombinant N/C-terminal 6... 39024966
Ephrin type-A receptor 2 IC50 = 5400.0 nM 5.27 Displacement of biotinylated Fc-tagged ephrin-A1 from C/N-terminal 6-His tagged ... 39024966
Ephrin type-B receptor 1 IC50 = 7700.0 nM 5.11 Displacement of biotinylated Fc-tagged ephrin-B1 from N/C-terminal recombinant r... 39024966
Ephrin type-B receptor 3 IC50 = 9800.0 nM 5.01 Displacement of biotinylated Fc-tagged ephrin-B1 from recombinant mouse EphB3 (L... 39024966
Ephrin type-B receptor 2 IC50 = 16000.0 nM 4.8 Displacement of biotinylated Fc-tagged ephrin-B1 from recombinant N/C-terminal 6... 39024966

Literature References

PubMed DOI Target Context # Activities
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 2 3
26363867 10.1016/j.ejmech.2015.08.048 Ephrin type-A receptor 2 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 1 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 3 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 4 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 5 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 6 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 7 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-A receptor 8 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-B receptor 1 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-B receptor 2 1
39024966 10.1016/j.ejmech.2024.116681 Ephrin type-B receptor 3 1

Data from ChEMBL 36 via Core Engine