SCHEMBL5223607

SCHEMBL5223607

O=C([O-])[C@@H](NCc1ccccc1)c1ccc(F)cc1.[Na+]

nearest known ligand 0.48

Known targets — ChEMBL curated mechanism

ABCC8ACEADORA1ADORA2AADORA2BADORA3ALDH5A1ALOX5ALOX5APATP4AATP4BBRAFCA1CA12CA2CA4CYSLTR1DHFRDPEP1EDNRAEDNRBESR2F10FDPSFGF1GABBR1GABBR2GABRA1GABRA2GABRA3GABRA4GABRA5GABRA6GABRB1GABRB2GABRB3GABRDGABREGABRG1GABRG2GABRG3GABRPGABRQGARTGNRHRGSC1HMGCRIMPDH1IMPDH2KCNJ11LY96NOD2NR3C1NS3NS4ANS5bP2RY1P2RY12P2RY2P2RY4P2RY6PBP2XPDE3APDE3BPDE4APDE4BPDE4CPDE4DPDK1PDK2PDK3PDK4PPARGPPATPTGIRPTGS1PTGS2RAF1RYR1RYR3SCN10ASCN11ASCN1ASCN2ASCN3ASCN4ASCN5ASCN7ASCN8ASCN9ASERPINC1SLC12A1SLC12A3SYKTHRATHRBTLR3TLR4TLR9TUBA1ATUBA1BTUBA1CTUBA3CTUBA3ETUBA4ATUBBTUBB1TUBB2ATUBB2BTUBB3TUBB4ATUBB4BTUBB6TUBB8TYMSVKORC1XDHblablaIMP-1blaOXA-33blaOXA-58blaT-3blaT-4blaT-5blaT-6dacAdacBdacCfolAfolPfolP1ftsIfusAgaggyrAgyrBmecAmrcAmrcBmrdApbp1apbp1bpbp2pbp2apbp2bpbp3pbp4pbpApbpBpbpCpbpFpolponBrplArplBrplCrplDrplErplFrplJrplKrplLrplMrplNrplOrplPrplQrplRrplSrplTrplUrplVrplWrplXrplYrpmArpmBrpmCrpmDrpmErpmFrpmGrpmHrpmIrpmJrpoArpoBrpoCrpoZrpsArpsBrpsCrpsDrpsErpsFrpsGrpsHrpsIrpsJrpsKrpsLrpsMrpsNrpsOrpsPrpsQrpsRrpsSrpsTrpsUykgMykgO

The experimentally established mechanism targets of None. 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
PPARG known ✓ P37231 1/20 0.41
CNR2 P34972 1/20 0.48
ALDH1A1 P00352 4/20 0.47
RAB9A P51151 2/20 0.47
MAPT P10636 2/20 0.46
CYP3A4 P08684 1/20 0.46
CYP2D6 P10635 1/20 0.46
CYP2C9 P11712 1/20 0.46
TSHR P16473 1/20 0.46
CYP2C19 P33261 1/20 0.46
KDM4E B2RXH2 2/20 0.46
MEN1 O00255 1/20 0.46
KMT2A Q03164 1/20 0.46
PLA2G1B P04054 1/20 0.43
ATG4B Q9Y4P1 1/20 0.43
LMNA P02545 2/20 0.43
NPC1 O15118 1/20 0.42
POLB P06746 1/20 0.42
MAOB P27338 1/20 0.42
MEP1B Q16820 2/20 0.42

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
SCHEMBL5224347 0.86 CNR2 (0.51) CNR2ALDH1A1RAB9AMAPTCYP3A4
SCHEMBL4427598 0.86 CNR2 (0.51) CNR2ALDH1A1RAB9AMAPTCYP3A4
SCHEMBL5223574 0.81 MEN1 (0.70) CNR2ALDH1A1RAB9AMAPTCYP3A4
SCHEMBL16664378 0.80 ALDH1A1 (0.50) ALDH1A1RAB9ACYP3A4CYP2D6CYP2C9
SCHEMBL2485602 0.80 ALDH1A1 (0.50) ALDH1A1RAB9ACYP3A4CYP2D6CYP2C9
Hydrochloric Acid SCHEMBL5224712 0.80 MEN1 (0.68) CNR2ALDH1A1RAB9AMAPTCYP3A4
Hydrochloric Acid SCHEMBL2484892 0.79 ALDH1A1 (0.49) ALDH1A1RAB9ACYP3A4CYP2D6CYP2C9
SCHEMBL4848539 0.75 CTSA (0.49) CNR2ALDH1A1RAB9AMAPTCYP3A4
SCHEMBL4848544 0.75 CTSA (0.49) CNR2ALDH1A1RAB9AMAPTCYP3A4
SCHEMBL4856270 0.75 CTSA (0.49) CNR2ALDH1A1RAB9AMAPTCYP3A4

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 19 patents. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-6432953-B1 None US disclosed
EP-0994867-B1 POLYMORPHIC FORM OF THE TACHYKININ RECEPTOR ANTAGONIST 2-(R)-(1-(R) -(3,5-BIS(TRIFLUOROMETHYL) PHENYL)ETHOXY)-3-(S)-(4-FLUORO) PHENYL-4-(3-5 (-OXO-1H,4H-1,2,4,-TRIAZOLO) METHYLMORPHOLINE MERCK & CO INC (US) 2007-09-12 EP disclosed
US-6638930-B2 Antiinflammatory agents, analgesics, antiasthmatics, antiemitics and calcium channel blockers for angina, hypertension or ischemia MERCK & CO. INC. 2003-10-28 US disclosed
US-6583142-B2 2-(R)-(1-(R)-(3,5- bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H -1,2,4-triazolo) methyl morpholine; antagonizing effect of substance P at its receptor site, blockade of neurokinin-1 receptors MERCK & CO. 2003-06-24 US disclosed
US-20030027825-A1 Polymorphic form of a tachykinin receptor antagonist MERCK & CO. INC. 2003-02-06 US disclosed
US-6432953-B2 2-(R)-(1-(R)-(3,5-BIS(TRIFLUOROMETHYL)-PHENYL)ETHOXY)-3-(S)-(4 -FLUORO) PHENYL-4-(3-(5-OXO-1H,4H-1,2,4-TRIAZOLO)METHYLMORPHOLINE; TREATING NEUROPATHY, EMESIS, NERVOUS SYSTEM DISORDERS; THERMODYNAMIC STABILITY FOR DRUGS MERCK & CO., INC. 2002-08-13 US disclosed
US-20020002164-A1 Morpholine and thiomorpholine tachykinin receptor antagonists MERCK & CO., INC. 2002-01-03 US disclosed
US-20010041702-A1 Polymorphic form of a tachykinin receptor antagonist MERCK & CO., INC. 2001-11-15 US disclosed
US-6235735-B1 AFTERTREATMENT OF RADIATION THERAPY MERCK & CO., INC. 2001-05-22 US disclosed
US-6229010-B1 RECOVERING FORM I OF 2-(R)-(1-(R)-(3,5-BIS(TRIFLUOROMETHYL) -PHENYL)ETHOXY)-3-(S)-(4-FLUORO)PHENYL-4-(3-(5-OXO-1H,4H-1,2,4 -TRIAZOLO)METHYLMORPHOLINE FROM FORM II EQUILIBRATED IN ETHANOL, ISOPROPANOL, ACETONITRILE OR ISOPROPYL ACETATE MERCK & CO., INC. 2001-05-08 US disclosed
US-6096742-A Polymorphic form of a tachykinin receptor antagonist MERCK & CO., INC. (US) 2000-08-01 US disclosed
EP-0994867-A1 POLYMORPHIC FORM OF THE TACHYKININ RECEPTOR ANTAGONIST 2-(R)-(1-(R) -(3,5-BIS(TRIFLUOROMETHYL) PHENYL)ETHOXY)-3-(S)-(4-FLUORO) PHENYL-4-(3-5 (-OXO-1H,4H-1,2,4,-TRIAZOLO) METHYLMORPHOLINE Merck & Co., Inc. (US) 2000-04-26 EP disclosed
US-6048859-A ANTIEMETIC AGENT MERCK & CO., INC. (US) 2000-04-11 US disclosed
US-5922706-A TREATING INFLAMMATORY DISEASES, PAIN OR MIGRAINE, ASTHMA AND EMESIS, AND CALCIUM CHANNEL BLOCKERS USEFUL IN THE TREATMENT OF CARDIOVASCULAR DISORDERS SUCH AS ANGINA, HYPERTENSION OR ISCHEMIA MERCK & CO., INC. (US) 1999-07-13 US disclosed
US-5872116-A TREATMENT OF INFLAMATION, PAIN, MIGRAINE, ASTHMA AND EMESIS MERCK & CO., INC. (US) 1999-02-16 US disclosed
WO-1999001444-A1 POLYMORPHIC FORM OF THE TACHYKININ RECEPTOR ANTAGONIST 2-(R)-(1-(R) -(3,5-BIS(TRIFLUOROMETHYL) PHENYL)ETHOXY)-3-(S)-(4-FLUORO) PHENYL-4-(3-5 (-OXO-1H,4H-1,2,4,-TRIAZOLO) METHYLMORPHOLINE MERCK & CO., INC. (US) 1999-01-14 WO disclosed
US-5780467-A USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES, PAIN OR MIGRAINE, ASTHMA AND EMESIS MERCK & CO., INC. (US) 1998-07-14 US disclosed
US-5719147-A Morpholine and thiomorpholine tachykinin receptor antagonists MERCK & CO., INC. (US) 1998-02-17 US disclosed
US-5691336-A ANTIINFLAMMATORY AGENTS; ANALGESICS; THERAPY OF ASTHMA, EMESIS MERCK & CO., INC. (US) 1997-11-25 US 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 (3 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-20020002164-A1 Morpholine and thiomorpholine tachykinin receptor antagonists TRPM7, TRPM2, TRPM5 PPARG 2345/4885CNR2 81/4885ALDH1A1 3320/4885
US-20010041702-A1 Polymorphic form of a tachykinin receptor antagonist OPRL1, MC3R, OPRK1 PPARG 3423/4885CNR2 119/4885ALDH1A1 3984/4885
US-20030027825-A1 Polymorphic form of a tachykinin receptor antagonist OPRL1, MC3R, MC5R PPARG 3395/4885CNR2 118/4885ALDH1A1 4047/4885

“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.