Trimetrexate

Trimetrexate

SCHEMBL7099424

CC(=O)O.COc1cc(NCc2ccc3nc(N)nc(N)c3c2C)cc(OC)c1OC

nearest known ligand 0.88

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

ADRA2AADRA2BADRA2CADRB2AGTR1AVPR1AAVPR1BAVPR2BDKRB2CALCRCHRNA3CHRNB4ESR1ESR2GHSRGNRHRGSC1HSPA8MALT1MC1RMC4RNOS1NOS2NOS3OPRK1OXTRRAMP1RAMP2RAMP3SCN5ASSTR1SSTR2SSTR3SSTR4SSTR5dacAdacBdacCfolPftsImrcAmrcBmrdArplArplBrplCrplDrplErplFrplJrplKrplLrplMrplNrplOrplPrplQrplRrplSrplTrplUrplVrplWrplXrplYrpmArpmBrpmCrpmDrpmErpmFrpmGrpmHrpmIrpmJrpsArpsBrpsCrpsDrpsErpsFrpsGrpsHrpsIrpsJrpsKrpsLrpsMrpsNrpsOrpsPrpsQrpsRrpsSrpsTrpsUykgMykgO

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
ESR1 known ✓ P03372 1/20 0.88
DHFR P00374 9/20 0.88
MEN1 O00255 1/20 0.88
ALDH1A1 P00352 1/20 0.88
CHRM2 P08172 1/20 0.88
HTR1A P08908 1/20 0.88
MAPT P10636 1/20 0.88
CHRM1 P11229 1/20 0.88
HPGD P15428 1/20 0.88
MAOA P21397 1/20 0.88
DRD1 P21728 1/20 0.88
ACHE P22303 1/20 0.88
PTGS1 P23219 1/20 0.88
SLC6A2 P23975 1/20 0.88
PDE4A P27815 1/20 0.88
OPRM1 P35372 1/20 0.88
DRD3 P35462 1/20 0.88
BLM P54132 1/20 0.88
SLC6A3 Q01959 1/20 0.88
KMT2A Q03164 1/20 0.88

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 SCHEMBL7099127 0.99 DHFR (0.86) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL29376841 0.94 DHFR (1.00) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL3983 0.94 DHFR (1.00) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL10701228 0.94 DHFR (1.00) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL29403928 0.94 DHFR (1.00) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL29906169 0.93 DHFR (0.98) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL7099341 0.93 DHFR (0.98) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL7099831 0.93 DHFR (0.98) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL7108746 0.92 DHFR (0.81) DHFRMEN1ALDH1A1ESR1CHRM2
Trimetrexate SCHEMBL8588679 0.92 DHFR (0.81) DHFRMEN1ALDH1A1ESR1CHRM2

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

PatentTitleAssigneePublishedPriorityFilingCountryStatus
CN-1152687-C Trimetrexate crystal and preparation method thereof E 2004-06-09 CN claimed
US-20030199694-A1 Thermally stable trimetrexates and processes for producing the same MEDIMMUNE ONCOLOGY, INC. 2003-10-23 US claimed
US-20020107393-A1 Tremextrexate derivatives and pharmaceutical compositions comprising the same MEDIMMUNE ONCOLOGY, INC. 2002-08-08 US claimed
EP-1080079-A4 THERMALLY STABLE TRIMETREXATES AND PROCESSES FOR PRODUCING THE SAME US BIOSCIENCE (US) 2001-10-04 EP claimed
US-6258952-B1 CRYSTALLIZATION MEDIMMUNE ONCOLOGY, INC. 2001-07-10 US claimed
EP-1080079-A1 THERMALLY STABLE TRIMETREXATES AND PROCESSES FOR PRODUCING THE SAME U.S. BIOSCIENCE, INC. (US) 2001-03-07 EP claimed
WO-1999059981-A1 THERMALLY STABLE TRIMETREXATES AND PROCESSES FOR PRODUCING THE SAME U.S. BIOSCIENCE, INC. (US) 1999-11-25 WO claimed
CN-1177925-A Trimetrexate crystal and preparation method thereof PAUL E KENNEDY (US) 1998-04-01 CN claimed
US-4391809-A Methods for treating psoriasis WARNER-LAMBERT COMPANY (US) 1983-07-05 US claimed
CN-1152687-C Trimetrexate crystal and preparation method thereof E 2004-06-09 CN disclosed
US-20030199694-A1 Thermally stable trimetrexates and processes for producing the same MEDIMMUNE ONCOLOGY, INC. 2003-10-23 US disclosed
US-20020107393-A1 Tremextrexate derivatives and pharmaceutical compositions comprising the same MEDIMMUNE ONCOLOGY, INC. 2002-08-08 US disclosed
EP-1080079-A4 THERMALLY STABLE TRIMETREXATES AND PROCESSES FOR PRODUCING THE SAME US BIOSCIENCE (US) 2001-10-04 EP disclosed
US-6258952-B1 CRYSTALLIZATION MEDIMMUNE ONCOLOGY, INC. 2001-07-10 US disclosed
WO-1996021451-A1 CRYSTALLINE TRIMETREXATE SALTS AND THE PROCESS FOR MAKING THE SAME KENNEDY PAUL E (US) 1996-07-18 WO disclosed
EP-0253396-B1 PROCESS FOR PREPARING 5,6-SUBSTITUTED-2,4-QUINAZOLINEDIAMINES AND INTERMEDIATES WARNER-LAMBERT COMPANY (US) 1993-03-17 EP disclosed
EP-0253396-A2 Process for preparing 5,6-substituted-2,4-quinazolinediamines and intermediates WARNER-LAMBERT COMPANY (US) 1988-01-20 EP disclosed
EP-0051415-B1 WATER-SOLUBLE SALTS OF 2,4-DIAMINO-5-METHYL-6-((3,4,5-TRIMETHOXYANILINO)METHYL)QUINAZOLINE, COMPOSITIONS CONTAINING SUCH SALTS AND THE PRODUCTION OF SUCH SALTS WARNER-LAMBERT COMPANY (US) 1984-11-14 EP disclosed
US-4376858-A TREATING MALARIA AND BACTERIAL INFECTIONS WARNER LAMBERT COMPANY (US) 1983-03-15 US disclosed
EP-0051415-A1 Water-soluble salts of 2,4-diamino-5-methyl-6-((3,4,5-trimethoxyanilino)methyl)quinazoline, compositions containing such salts and the production of such salts WARNER-LAMBERT COMPANY (US) 1982-05-12 EP 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-20030199694-A1 Thermally stable trimetrexates and processes for producing the same TYMS, TYMP, TOP1 ESR1 4342/4885DHFR 107/4885MEN1 2297/4885
US-20020107393-A1 Tremextrexate derivatives and pharmaceutical compositions comprising the same TYMP, TYMS, DTYMK ESR1 3290/4885DHFR 147/4885MEN1 2476/4885

“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.