Befetupitant

Befetupitant

SCHEMBL1469769

Cc1ccccc1-c1cc(N2CCOCC2)ncc1N(C)C(=O)C(C)(C)c1cc(C(F)(F)F)cc(C(F)(F)F)c1.Cl

nearest known ligand 0.98

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

ABL1ACEACHEACVR1ADRA1AADRA1BADRA1DADRA2AADRA2BADRA2CADRB1ADRB2ADRB3AGTR1ALKAVPR1AAVPR2BCHEBCRCA2CACNA1ACACNA1BCACNA1CCACNA1DCACNA1ECACNA1FCACNA1GCACNA1HCACNA1ICACNA1SCACNA2D1CACNA2D2CACNA2D3CACNA2D4CACNB1CACNB2CACNB3CACNB4CACNG1CACNG2CACNG3CACNG4CACNG5CACNG6CACNG7CACNG8CALCRLCASRCCR5CDK4CDK6CFBCHRM1CHRM2CHRM3CHRM4CHRM5CHRNA1CHRNA3CHRNA7CHRNB1CHRNB4CHRNDCHRNECHRNGCOXFA4COXFA4L2CRBNCSF1RCUL4ACYP19A1DDB1DPP4DRD1DRD2DRD3DRD4EDNRAEGFREML4ERBB2ERBB4ESR1ESR2FGFR1FGFR3FLT1FLT3FLT4GAAGABRA1GABRA2GABRA3GABRA4GABRA5GABRA6GABRB1GABRB2GABRB3GABRDGABREGABRG1GABRG2GABRG3GABRPGABRQGHSRGLAGNRHRGPD2GRIN1GRIN2AGRIN2BGRIN2CGRIN2DGRIN3AGRIN3BGSTP1HCN4HCRTR1HCRTR2HDAC1HDAC10HDAC11HDAC2HDAC3HDAC4HDAC5HDAC6HDAC7HDAC8HDAC9HRH1HRH2HRH3HSD11B1HSP90AA1HSP90AB1HTR1AHTR1BHTR1DHTR1EHTR1FHTR2AHTR2BHTR2CHTR3AHTR3BHTR3CHTR3DHTR3EHTR4HTR5AHTR6HTR7IMPDH1IMPDH2ITGA2BITGB3ITKJAK1JAK2KCNA1KCNA10KCNA2KCNA3KCNA4KCNA5KCNA6KCNA7KCNB1KCNB2KCNC1KCNC2KCNC3KCNC4KCND1KCND2KCND3KCNF1KCNG1KCNG2KCNG3KCNG4KCNH1KCNH2KCNH3KCNH4KCNH5KCNH6KCNH7KCNH8KCNJ2KCNJ3KCNJ5KCNK3KCNK9KCNQ1KCNQ2KCNQ3KCNQ4KCNQ5KCNS1KCNS2KCNS3KCNV1KCNV2KDRKITKLKB1LCKMMAOAMAOBMAPK14METMMP1MMP13MMP7MMP8MT-ND1MT-ND2MT-ND3MT-ND4MT-ND4LMT-ND5MT-ND6NDUFA1NDUFA10NDUFA11NDUFA12NDUFA13NDUFA2NDUFA3NDUFA5NDUFA6NDUFA7NDUFA8NDUFA9NDUFAB1NDUFAF1NDUFAF2NDUFAF3NDUFAF4NDUFB1NDUFB10NDUFB11NDUFB2NDUFB3NDUFB4NDUFB5NDUFB6NDUFB7NDUFB8NDUFB9NDUFC1NDUFC2NDUFS1NDUFS2NDUFS3NDUFS4NDUFS5NDUFS6NDUFS7NDUFS8NDUFV1NDUFV2NDUFV3NR3C1NS5ANTRK1NTRK2NTRK3ODC1OPRD1OPRK1OPRM1P2RY12PAHPARP1PDE3APDE3BPDE4APDE4BPDE4CPDE4DPDE5APDE7APDE7BPDE8APDE8BPDGFRAPDGFRBPIK3CAPIK3CDPNPPOLA1POLA2POLD1POLD2POLD3POLD4POLEPOLE2POLE3PPARGPRIM1PRIM2PRKCAPRKCBPRKCDPRKCEPRKCGPRKCHPRKCIPRKCQPRKCZPRKD1PRKD3PTGS1PTGS2RBX1RENRETROCK1ROCK2RPE65RRM1RRM2RRM2BS1PR1S1PR2S1PR3S1PR4S1PR5SCN10ASCN11ASCN1ASCN2ASCN3ASCN4ASCN5ASCN7ASCN8ASCN9ASCNN1ASCNN1BSCNN1GSIGMAR1SLC18A2SLC6A1SLC6A2SLC6A3SLC6A4SLC9A3SRCTACR1TOP1TOP2ATOP2BTTRTYMPdacAdacBdacCembAfolAftsIgyrAgyrBmrcAmrcBmrdAparCparEpolrplArplBrplCrplDrplErplFrplIrplJrplKrplLrplMrplNrplOrplPrplQrplRrplSrplTrplUrplVrplWrplXrplYrpmArpmBrpmCrpmDrpmErpmE2rpmFrpmGrpmG1rpmG2rpmG3rpmHrpmIrpmJrpsArpsBrpsCrpsDrpsErpsFrpsGrpsHrpsIrpsJrpsKrpsLrpsMrpsNrpsOrpsPrpsQrpsRrpsSrpsTrpsUykgMykgO

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

Predicted protein targets (top 4)

geneUniProtsupporting neighboursconfidence
TACR1 known ✓ P25103 19/20 0.98
CYP3A4 P08684 4/20 0.73
TACR3 P29371 6/20 0.62
GPBAR1 Q8TDU6 1/20 0.60

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
Befetupitant SCHEMBL29374667 0.99 TACR1 (1.00) TACR1CYP3A4TACR3GPBAR1
Befetupitant SCHEMBL1399438 0.99 TACR1 (1.00) TACR1CYP3A4TACR3GPBAR1
Hydrochloric Acid SCHEMBL6633807 0.91 TACR1 (0.81) TACR1CYP3A4TACR3
Netupitant SCHEMBL30800106 0.90 TACR1 (0.98) TACR1CYP3A4TACR3GPBAR1
Netupitant SCHEMBL6637560 0.90 TACR1 (0.98) TACR1CYP3A4TACR3GPBAR1
Netupitant SCHEMBL17222804 0.90 TACR1 (0.98) TACR1CYP3A4TACR3GPBAR1
SCHEMBL13593642 0.90 TACR1 (0.84) TACR1CYP3A4TACR3GPBAR1
SCHEMBL2184409 0.90 TACR1 (0.82) TACR1CYP3A4TACR3
Netupitant SCHEMBL445804 0.90 TACR1 (1.00) TACR1CYP3A4TACR3GPBAR1
Netupitant SCHEMBL29809811 0.90 TACR1 (1.00) TACR1CYP3A4TACR3GPBAR1

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

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-20130189362-A1 NOVEL DOSAGE FORMULATION HOFFMANN-LA ROCHE INC. (US) 2013-07-25 US claimed
US-20110070303-A1 NOVEL DOSAGE FORMULATION AHMED HASHIM A 2011-03-24 US claimed
EP-1928427-B1 NOVEL DOSAGE FORMULATION HOFFMANN LA ROCHE (CH) 2009-12-30 EP claimed
EP-1928427-A1 NOVEL DOSAGE FORMULATION F.HOFFMANN-LA ROCHE AG (CH) 2008-06-11 EP claimed
WO-2007039420-A1 NOVEL DOSAGE FORMULATION F. HOFFMANN-LA ROCHE AG (CH) 2007-04-12 WO claimed
US-20070071813-A1 Novel dosage formulation AHMED HASHIM A 2007-03-29 US claimed
US-8852634-B2 Dosage formulation HOFFMANN-LA ROCHE INC. (US) 2014-10-07 US disclosed
US-20130189362-A1 NOVEL DOSAGE FORMULATION HOFFMANN-LA ROCHE INC. (US) 2013-07-25 US disclosed
US-20110070303-A1 NOVEL DOSAGE FORMULATION AHMED HASHIM A 2011-03-24 US disclosed
EP-1928427-B1 NOVEL DOSAGE FORMULATION HOFFMANN LA ROCHE (CH) 2009-12-30 EP disclosed
EP-1928427-A1 NOVEL DOSAGE FORMULATION F.HOFFMANN-LA ROCHE AG (CH) 2008-06-11 EP disclosed
WO-2007039420-A1 NOVEL DOSAGE FORMULATION F. HOFFMANN-LA ROCHE AG (CH) 2007-04-12 WO disclosed
US-20070071813-A1 Novel dosage formulation AHMED HASHIM A 2007-03-29 US disclosed
EP-1394150-A1 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists F. HOFFMANN-LA ROCHE AG (CH) 2004-03-03 EP disclosed
EP-1103545-B1 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide HOFFMANN LA ROCHE (CH) 2003-11-05 EP disclosed
US-6479483-B2 3,4,6-SUBSTITUTED PYRIDINE DERIVATIVES USEFUL FOR TREATING DEPRESSION AND PAIN, RESULTING FROM INFLAMMATORY CONDITIONS, SUCH AS MIGRAINE, RHEUMATOID ARTHRITIS, ASTHMA AND INFLAMATORY BOWEL DISEASE; NK1 RECEPTOR ANTAGONIST HOFFMANN-LA ROCHE INC. 2002-11-12 US disclosed
US-20020091265-A1 4-phenyl-pyridine derivatives BOS MICHAEL (CA) 2002-07-11 US disclosed
US-6297375-B1 4-phenyl-pyridine derivatives HOFFMANN-LA ROCHE INC. 2001-10-02 US disclosed
EP-1103545-A1 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide F. HOFFMANN-LA ROCHE AG (CH) 2001-05-30 EP disclosed
EP-1035115-A1 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists F. HOFFMANN-LA ROCHE AG (CH) 2000-09-13 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 (4 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-20130189362-A1 NOVEL DOSAGE FORMULATION ABCB11, F12, CYP4A11 TACR1 2804/4885CYP3A4 68/4885TACR3 4459/4885
US-20110070303-A1 NOVEL DOSAGE FORMULATION ABCB11, F12, CYP4A11 TACR1 2804/4885CYP3A4 68/4885TACR3 4459/4885
US-20070071813-A1 Novel dosage formulation ABCB11, F12, CYP4A11 TACR1 2804/4885CYP3A4 68/4885TACR3 4459/4885
US-20020091265-A1 4-phenyl-pyridine derivatives CBR1, CBR3, HCCS TACR1 534/4885CYP3A4 908/4885TACR3 551/4885

“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.