Trimetrexate

Trimetrexate

SCHEMBL166271

COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC.Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)C2(F)F)c(=O)n1

nearest known ligand 0.58

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

POLA1POLA2POLD1POLD2POLD3POLD4POLEPOLE2POLE3PRIM1PRIM2RRM1RRM2RRM2B

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

Predicted protein targets (top 20)

geneUniProtsupporting neighboursconfidence
POLA1 known ✓ P09884 2/20 0.42
DHFR P00374 8/20 0.58
PDE3A Q14432 2/20 0.58
MEN1 O00255 1/20 0.58
ALDH1A1 P00352 1/20 0.58
ESR1 P03372 1/20 0.58
CHRM2 P08172 1/20 0.58
HTR1A P08908 1/20 0.58
MAPT P10636 1/20 0.58
CHRM1 P11229 1/20 0.58
HPGD P15428 1/20 0.58
MAOA P21397 1/20 0.58
DRD1 P21728 1/20 0.58
ACHE P22303 1/20 0.58
PTGS1 P23219 1/20 0.58
SLC6A2 P23975 1/20 0.58
PDE4A P27815 1/20 0.58
OPRM1 P35372 1/20 0.58
DRD3 P35462 1/20 0.58
BLM P54132 1/20 0.58

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
Trimetrexate SCHEMBL5056582 0.79 DHFR (0.60) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL19100456 0.78 DHFR (0.59) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL28146995 0.77 DHFR (0.68) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL10701228 0.76 DHFR (1.00) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL7099831 0.75 DHFR (0.98) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL7099341 0.75 DHFR (0.98) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL28151291 0.75 DHFR (0.70) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL8039650 0.75 DHFR (0.88) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL28142980 0.75 DHFR (0.88) DHFRPDE3AMEN1ALDH1A1ESR1
Trimetrexate SCHEMBL7099424 0.75 DHFR (0.88) DHFRPDE3AMEN1ALDH1A1ESR1

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 69 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
EP-3672952-A1 BEZIMIDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS Merck Patent GmbH (DE) 2020-07-01 EP disclosed
EP-3672951-A1 QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS Merck Patent GmbH (DE) 2020-07-01 EP disclosed
EP-3668516-A1 STABLE LYOPHILISATES COMPRISING 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID AND A DICARBOXYLIC ACID Merck Patent GmbH (DE) 2020-06-24 EP disclosed
EP-3661941-A1 THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS Merck Patent GmbH (DE) 2020-06-10 EP disclosed
WO-2019038215-A1 BEZIMIDAZOLE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS MERCK PATENT GMBH (DE) 2019-02-28 WO disclosed
WO-2019038214-A1 QUINOXALINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS MERCK PATENT GMBH (DE) 2019-02-28 WO disclosed
WO-2019034673-A1 STABLE LYOPHILISATES COMPRISING 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID AND A DICARBOXYLIC ACID MERCK PATENT GMBH (DE) 2019-02-21 WO disclosed
WO-2019025099-A1 THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR ANTAGONISTS MERCK PATENT GMBH (DE) 2019-02-07 WO disclosed
EP-2994471-A1 MACROCYCLES AS KINASE INHIBITORS Merck Patent GmbH (DE) 2016-03-16 EP disclosed
EP-2976328-A1 PIPERAZINE DERIVATIVES AS FASN INHIBITORS Merck Patent GmbH (DE) 2016-01-27 EP disclosed
EP-2352732-A1 2, 5-DIAMINO-SUBSTITUTED PYRIDO Ý4, 3-D¨PYRIMIDINES AS AUTOTAXIN INHIBITORS AGAINST CANCER Merck Patent GmbH (DE) 2011-08-10 EP disclosed
EP-2254889-A1 PROTEIN KINASE INHIBITORS AND USE THEREOF Merck Patent GmbH (DE) 2010-12-01 EP disclosed
WO-2010115491-A2 PIPERIDINE AND PIPERAZINE DERIVATIVES AS AUTOTAXIN INHIBITORS MERCK PATENT GMBH (DE) 2010-10-14 WO disclosed
WO-2010112124-A1 AUTOTAXIN INHIBITORS MERCK PATENT GMBH (DE) 2010-10-07 WO disclosed
WO-2010078897-A1 NOVEL POLYMORPHIC FORMS OF 3-(1-{3-[5-(1-METHYL-PIPERIDIN-4YLMETHOXY)-PYRIMIDIN-2-YL]-BENZYL}-6-OXO-1,6-DIHYDRO-PYRIDAZIN-3-YL)-BENZONITRILE HYDROCHLORIDE SALT AND PROCESSES OF MANUFACTURING THEREOF MERCK PATENT GMBH (DE) 2010-07-15 WO disclosed
WO-2010080253-A1 TRICYCLIC AZAINDOLES MERCK PATENT GMBH (DE) 2010-07-15 WO disclosed
WO-2010077530-A1 C-RING MODIFIED TRICYCLIC BENZONAPHTHIRIDINONE PROTEIN KINASE INHIBITORS AND USE THEREOF MERCK PATENT GMBH (DE) 2010-07-08 WO disclosed
WO-2010072295-A1 NOVEL POLYMORPHIC FORMS OF 6-(1-METHYL-1H-PYRAZOL-4-YL)-2-{3-[5-(2-MORPHOLIN-4-YL-ETHOXY)-PYRIMIDIN-2-YL]-BENZYL}-2H-PYRIDAZIN-3-ONE DIHYDROGENPHOSPHATE AND PROCESSES OF MANUFACTURING THEREOF MERCK PATENT GMBH (DE) 2010-07-01 WO disclosed
WO-2010063352-A1 2, 5-DIAMINO-SUBSTITUTED PYRIDO [4, 3-D] PYRIMIDINES AS AUTOTAXIN INHIBITORS AGAINST CANCER MERCK PATENT GMBH (DE) 2010-06-10 WO disclosed
WO-2009108670-A1 PROTEIN KINASE INHIBITORS AND USE THEREOF MERCK SERONO S.A. (CH) 2009-09-03 WO disclosed