Gyki-52466

Gyki-52466

SCHEMBL249675

CC1=NN=C(c2ccc(N)cc2)c2cc3c(cc2C1)OCO3.Cl

nearest known ligand 1.00 ✓ in ChEMBL — recovers established targets

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 Gyki-52466. 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
LMNA P02545 2/20 1.00
GRIA2 P42262 4/20 0.97
MEN1 O00255 2/20 0.97
CYP1A2 P05177 2/20 0.97
CYP3A4 P08684 2/20 0.97
CYP2D6 P10635 2/20 0.97
MAPT P10636 2/20 0.97
CYP2C9 P11712 2/20 0.97
NFKB1 P19838 2/20 0.97
CYP2C19 P33261 2/20 0.97
KMT2A Q03164 2/20 0.97
HIF1A Q16665 2/20 0.97
ALDH1A1 P00352 1/20 0.97
TDP1 Q9NUW8 1/20 0.97
ALOX15 P16050 1/20 0.54
MAPK1 P28482 1/20 0.54
HSD17B10 Q99714 1/20 0.54
KDM4E B2RXH2 1/20 0.54
BLM P54132 1/20 0.54
PMP22 Q01453 1/20 0.54

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
Gyki-52466 SCHEMBL29651319 1.00 LMNA (1.00) LMNAGRIA2MEN1CYP1A2CYP3A4
Gyki-52466 SCHEMBL25227675 1.00 LMNA (1.00) LMNAGRIA2MEN1CYP1A2CYP3A4
Gyki-52466 SCHEMBL29357520 0.99 GRIA2 (1.00) LMNAGRIA2MEN1CYP1A2CYP3A4
Gyki-52466 SCHEMBL194854 0.99 GRIA2 (1.00) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL10887479 0.85 GRIA2 (0.76) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL7492463 0.81 MAPT (0.69) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL350464 0.80 GRIA2 (0.68) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL7164964 0.80 GRIA2 (0.68) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL8795316 0.80 GRIA2 (0.67) LMNAGRIA2MEN1CYP1A2CYP3A4
SCHEMBL5048632 0.80 GRIA2 (0.67) LMNAGRIA2MEN1CYP1A2CYP3A4

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

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-20110244486-A1 METHODS AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF DIABETES PEREGO, CARLA (IT) 2011-10-06 US claimed
EP-2366106-A2 METHODS AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF DIABETES Perego, Carla (IT) 2011-09-21 EP claimed
WO-2010057647-A2 METHODS AND COMPOSITIONS FOR THE DIAGNOSIS AND TREATMENT OF DIABETES UNIVERSITA' DEGLI STUDI DI MILANO (IT) 2010-05-27 WO claimed
EP-0778023-B1 Product comprising rapamycin or particular derivatives and an NMDA or AMPA antagonist for use for the treatment of epilepsy or Huntington's Disease, and the use of rapamycin or particular derivatives for the manufacture of a medicament for the treatment of epilepsy or Huntington's Disease. WYETH CORP (US) 2003-03-12 EP claimed
US-20030045449-A1 Pharmaceutical combinations for the treatment of neurodegenerative diseases PFIZER, INC. 2003-03-06 US claimed
EP-0778023-A1 Neuroprotective agents AMERICAN HOME PRODUCTS CORPORATION (US) 1997-06-11 EP claimed
US-20200030304-A1 MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS THE REGENTS OF THE UNIVERSITY OF CALIFORNIA 2020-01-30 US disclosed
US-10485814-B2 Nicotinamide riboside analogs and pharmaceutical compositions and uses thereof GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED (GB) 2019-11-26 US disclosed
US-10316054-B2 Preparation and use of crystalline beta-D-nicotinamide riboside GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED (GB) 2019-06-11 US disclosed
WO-2018169798-A9 MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS THE REGENTS OF THE UNIVERSITY OF CALIFORNIA (US) 2018-10-18 WO disclosed
WO-2018169798-A1 MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS THE REGENTS OF THE UNIVERSITY OF CALIFORNIA (US) 2018-09-20 WO disclosed
WO-2018066701-A1 PROPHYLACTIC OR THERAPEUTIC AGENT FOR FTLD AND METHOD FOR SCREENING SAME 国立大学法人京都大学 2018-04-12 WO disclosed
WO-2018033639-A1 LACTONE INTERMEDIATES OF NICOTINAMIDE RIBOSIDE AND NICOTINATE RIBOSIDE THE QUEEN'S UNIVERSITY OF BELFAST (GB) 2018-02-22 WO disclosed
US-20020045656-A1 Pharmaceutical combinations for the treatment of stroke and traumatic brain injury CHENARD BERTRAND L (US) 2002-04-18 US disclosed
EP-1186303-A2 Pharmaceutical combinations, for the treatment of stroke and traumatic brain injury, containing a neutrophil inhibiting factor and an selective NMDA-NR2B receptor antagonist Pfizer Products Inc. (US) 2002-03-13 EP disclosed
EP-1186304-A2 Pharmaceutical combinations for the treatment of stroke and traumatic brain injury Pfizer Products Inc. (US) 2002-03-13 EP disclosed
EP-1021418-A4 SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONES AND THE USE THEREOF COCENSYS INC (US) 2001-06-13 EP disclosed
EP-1021418-A1 SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONES AND THE USE THEREOF Cocensys, Inc. (US) 2000-07-26 EP disclosed
US-5891871-A 2-AMINO-3-(3-HYDROXY-5-METHYLISOXAZ-4-YL)PROPIONIC ACID RECEPTOR ANTAGONISTS; TREATING NEURONAL LOSS ASSOCIATED WITH STROKE, ISCHEMIA, CNS TRAUMA, HYPOGLYCEMIA OR SURGERY; OR TREATING NEURODEGENERATIVE DISEASES. COCENSYS, INC. (US) 1999-04-06 US disclosed
WO-1997034878-A1 SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONES AND THE USE THEREOF COCENSYS, INC. (US) 1997-09-25 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 (5 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-20200030304-A1 MITIGATION OF CNS DISORDERS BY COMBINATION THERAPY USING NEUROSTEROIDS, AND AMPA BLOCKERS GABRA4, GABRG1, GABRB2 LMNA 4011/4885GRIA2 58/4885MEN1 1957/4885
US-20030045449-A1 Pharmaceutical combinations for the treatment of neurodegenerative diseases GRIN3A, GRIN1, CHRNA10 LMNA 1289/4885GRIA2 167/4885MEN1 3328/4885
US-20020045656-A1 Pharmaceutical combinations for the treatment of stroke and traumatic brain injury GABRP, GRIN3B, GRIN1 LMNA 3004/4885GRIA2 66/4885MEN1 4183/4885
US-10316054-B2 Preparation and use of crystalline beta-D-nicotinamide riboside NNT, HADHB, NAMPT LMNA 393/4885GRIA2 4581/4885MEN1 2090/4885
US-10485814-B2 Nicotinamide riboside analogs and pharmaceutical compositions and uses thereof NNT, CS, ME2 LMNA 515/4885GRIA2 3454/4885MEN1 1467/4885

“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.