Compound Detail
CHEMBL1952329
SGI-1776 Phase I
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Phase I
Basic Information
| ChEMBL ID | CHEMBL1952329 |
| Name | SGI-1776 |
| Phase | Phase I |
| Structure Type | MOL |
| InChI Key | MHXGEROHKGDZGO-UHFFFAOYSA-N |
27
Targets
74
Activities
4
Assay Types
0
PK Parameters
20
Publications
1
Known Names
3
Indications
1
Mechanisms
Molecular Properties
405.4
MW (Da)
4.05
ALogP
6
HBA
1
HBD
54.7
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serine/threonine-protein kinase PIM inhibitor | INHIBITOR | Serine/threonine-protein kinase PIM | ✓ | ✓ |
Indications
Leukemia Lymphoma, Non-Hodgkin Prostatic Neoplasms, Castration-Resistant
Activity Summary
IC50 50 meas. best 8.15
Kd 15 meas. best 7.64
Ki 7 meas. best 7.92
EC50 2 meas. best 6.7
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Serine/threonine-protein kinase pim-1 CHEMBL2147 | IC50 | 8.15 | 7.9717 | 7.0 | 18 |
| Serine/threonine-protein kinase pim-1 CHEMBL2147 | Ki | 7.92 | 7.84 | 12.0 | 3 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | IC50 | 7.68 | 7.44 | 21.0 | 4 |
| 5'-AMP-activated protein kinase subunit gamma-2 CHEMBL2453 | Kd | 7.64 | 7.64 | 23.0 | 1 |
| Serine/threonine-protein kinase pim-3 CHEMBL5407 | Ki | 7.62 | 7.62 | 24.0 | 2 |
| Interleukin-1 receptor-associated kinase 3 CHEMBL5081 | Kd | 7.58 | 7.58 | 26.0 | 1 |
| MV4-11 CHEMBL613835 | IC50 | 7.52 | 7.52 | 30.0 | 1 |
| Serine/threonine-protein kinase haspin CHEMBL1075163 | IC50 | 7.47 | 7.47 | 34.0 | 1 |
| Serine/threonine-protein kinase pim-2 CHEMBL4523 | IC50 | 7.44 | 6.5363 | 36.3 | 8 |
| Serine/threonine-protein kinase pim-1 CHEMBL2147 | Kd | 7.37 | 7.37 | 43.0 | 1 |
| Serine/threonine-protein kinase pim-3 CHEMBL5407 | IC50 | 7.3 | 7.18 | 50.5 | 7 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | Kd | 6.84 | 6.84 | 143.0 | 1 |
| Serine/threonine-protein kinase pim-1 CHEMBL2147 | EC50 | 6.7 | 6.7 | 200.0 | 1 |
| Tyrosine-protein kinase Yes CHEMBL2073 | IC50 | 6.62 | 6.095 | 240.0 | 2 |
| Activin receptor type-1 CHEMBL5903 | Kd | 6.34 | 6.34 | 458.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.29 | 6.1 | 511.0 | 3 |
| Unchecked CHEMBL612545 | IC50 | 6.22 | 6.22 | 600.0 | 1 |
| Serine/threonine-protein kinase pim-2 CHEMBL4523 | Ki | 6.21 | 6.21 | 610.0 | 2 |
| Platelet-derived growth factor receptor beta CHEMBL1913 | Kd | 5.79 | 5.79 | 1607.0 | 1 |
| WI-38 CHEMBL614391 | IC50 | 5.77 | 5.77 | 1700.0 | 1 |
| Serine/threonine-protein kinase 10 CHEMBL3981 | Kd | 5.67 | 5.67 | 2159.0 | 1 |
| K562 CHEMBL385 | IC50 | 5.64 | 5.64 | 2290.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 5.49 | 5.49 | 3217.0 | 1 |
| STE20-like serine/threonine-protein kinase CHEMBL4202 | Kd | 5.45 | 5.45 | 3588.0 | 1 |
| PC-3 CHEMBL390 | IC50 | 5.32 | 5.32 | 4830.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 5.31 | 5.31 | 4860.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | EC50 | 5.3 | 5.3 | 5000.0 | 1 |
| Serine/threonine-protein kinase SIK2 CHEMBL5699 | Kd | 5.21 | 5.21 | 6124.0 | 1 |
| LNCaP CHEMBL612518 | IC50 | 5.16 | 5.16 | 6850.0 | 1 |
| Casein kinase II subunit alpha' CHEMBL4070 | Kd | 5.1 | 5.1 | 7924.0 | 1 |
| BMP-2-inducible protein kinase CHEMBL4522 | Kd | 5.07 | 5.07 | 8535.0 | 1 |
| Cyclin-G-associated kinase CHEMBL4355 | Kd | 5.06 | 5.06 | 8634.0 | 1 |
| Ribosomal protein S6 kinase alpha-6 CHEMBL4924 | Kd | 4.62 | 4.62 | 23762.0 | 1 |
| Serine/threonine-protein kinase N1 CHEMBL3384 | Kd | 4.45 | 4.45 | 35424.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine