Glpg-0259

Glpg-0259

SCHEMBL1889564

CC(C)N1C[C@H]2C[C@@H]1CN2c1ccc(Nc2ncc(-c3coc(C(N)=O)c3)n3ncnc23)cc1

nearest known ligand 0.49

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

MAPKAPK5

The experimentally established mechanism targets of Glpg-0259. The predicted profile below is derived independently by chemical similarity — agreement is a validation signal, a miss is honest.

Predicted protein targets (top 8)

geneUniProtsupporting neighboursconfidence
MAPKAPK5 known ✓ Q8IW41 11/20 0.49
SYK P43405 1/20 0.41
TTK P33981 1/20 0.33
MAP3K12 Q12852 1/20 0.32
BTK Q06187 1/20 0.31
TLR9 Q9NR96 2/20 0.30
TLR8 Q9NR97 2/20 0.30
TLR7 Q9NYK1 2/20 0.30

Click a target to see other patent compounds predicted against it — the reverse direction, in place.

Similar compounds — the chemically nearest patent molecules

Nearest neighbours by Morgan-fingerprint cosine across the patent-compound collection, with each neighbour's top predicted target and the predicted targets it shares with this molecule.

Compoundsimilaritytop predictedshared targets
Glpg-0259 SCHEMBL1570157 1.00 MAPKAPK5 (0.49) MAPKAPK5SYKTTKMAP3K12BTK
Glpg-0259 SCHEMBL12661679 1.00 MAPKAPK5 (0.49) MAPKAPK5SYKTTKMAP3K12BTK
SCHEMBL1570061 0.94 MAPKAPK5 (0.49) MAPKAPK5SYKTTKBTK
SCHEMBL1570224 0.92 MAPKAPK5 (0.42) MAPKAPK5SYKTTKMAP3K12
SCHEMBL2389923 0.91 MAPKAPK5 (0.42) MAPKAPK5SYKTTKMAP3K12BTK
SCHEMBL2390918 0.89 MAPKAPK5 (0.48) MAPKAPK5SYKBTK
SCHEMBL2390549 0.89 MAPKAPK5 (0.48) MAPKAPK5SYKBTK
SCHEMBL2389877 0.87 MAPKAPK5 (0.64) MAPKAPK5SYKTTK
SCHEMBL1570213 0.84 MAPKAPK5 (0.49) MAPKAPK5SYKTTK
SCHEMBL1570149 0.84 MAPKAPK5 (0.53) MAPKAPK5SYKTTK

Similarity is cosine over the 2,048-bit Morgan fingerprint (≈ Tanimoto). Identical fingerprints score 1.00.

Patent provenance — the patents this molecule appears in, and who filed them

Claimed or disclosed in 11 patents. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-8012983-B2 Substituted triazolopyrazines useful for the treatment of degenerative and inflammatory diseases GALAPAGOS NV (BE) 2011-09-06 US disclosed
US-8012983-B2 Substituted triazolopyrazines useful for the treatment of degenerative and inflammatory diseases GALAPAGOS NV (BE) 2011-09-06 US disclosed
US-8012983-B2 Substituted triazolopyrazines useful for the treatment of degenerative and inflammatory diseases GALAPAGOS NV (BE) 2011-09-06 US disclosed
US-20110118269-A1 FUSED PYRAZINE COMPOUNDS AS THEIR SALTS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS N.V. (BE) 2011-05-19 US disclosed
US-20110118269-A1 FUSED PYRAZINE COMPOUNDS AS THEIR SALTS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS N.V. (BE) 2011-05-19 US disclosed
US-20110118269-A1 FUSED PYRAZINE COMPOUNDS AS THEIR SALTS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS N.V. (BE) 2011-05-19 US disclosed
WO-2011054922-A1 SALTS OF FUSED PYRAZINE COMPOUNDS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES. GALAPAGOS NV (BE) 2011-05-12 WO disclosed
US-20090286798-A1 FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS NV (BE) 2009-11-19 US disclosed
US-20090286798-A1 FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS NV (BE) 2009-11-19 US disclosed
US-20090286798-A1 FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS NV (BE) 2009-11-19 US disclosed
WO-2009135885-A1 FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES GALAPAGOS NV (BE) 2009-11-12 WO disclosed

Patent text — is the patent's own abstract consistent with the prediction?

For each of this compound's patents that has machine-readable text (2 of them — usually the abstract, not the full specification), we ask MedCPT which protein the text reads most about, and where the chemistry-predicted target lands among 4885 human targets. A high rank means the patent's own wording is consistent with the prediction — a weak, independent signal, not proof of activity.

PatentTitleText reads most aboutPredicted target · text-rank
US-20110118269-A1 FUSED PYRAZINE COMPOUNDS AS THEIR SALTS, USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES IL1B, IL1A, NLRP3 MAPKAPK5 89/4885SYK 2268/4885TTK 3511/4885
US-20090286798-A1 FUSED PYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES IL1B, IL1A, PTGER1 MAPKAPK5 131/4885SYK 3339/4885TTK 3810/4885

“Text reads most about” is the patent abstract's nearest protein in MedCPT space (background-debiased). Only ~1.4% of patents have machine-readable text, so most compounds won't have this panel.