BDBM163654 MbA-CR (8)
US10106501, Example CR BDBM293219
BDBM50624835 Ls-104 Tyrene cr-4
BDBM50331515 PAROXETINE CHEMBL1708 Paroxetine hydrochloride Paxil cr Paroxetine.HCl Paxil
Dynacirc ISRADIPINE Isrodipine Dynacirc Cr PN-200-110 BDBM50436176
4-(3,4-Dichloro-benzoylamino)-4-dipentylcarbamoyl-butyric acid BDBM50005459 CR 1409 CHEMBL9485
Afeditab Cr CHEBI:7565 Procardia Xl Adalat Cc BAY-A-1040 BDBM50101817 Adalat Procardia Nifedipine
(nifedipine) 2,6-Dimethyl-4-(2-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester Afeditab cr Procardia XL 2,6-Dimethyl-4-(2-nitro-phenyl)-1,4-dihydro-pyridine-3,5-dicarboxylic acid dimethyl ester dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Adalat CC BAY-A-1040 NIFEDIPINE Adalat Nefidipine BDBM50336640 Procardia
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- ChEBML_90277 Inhibition of insulin receptor autophosphorylation
- ChEMBL_334490 (CHEMBL862525) Inhibition of insulin receptor
- ChEMBL_377345 (CHEMBL865408) Inhibition of Insulin receptor
- ChEMBL_506205 (CHEMBL941409) Inhibition of insulin receptor
- ChEMBL_581990 (CHEMBL1058970) Inhibition of insulin receptor
- ChEMBL_635332 (CHEMBL1119645) Inhibition of insulin receptor
- ChEMBL_698757 (CHEMBL1648482) Inhibition of insulin receptor
- ChEMBL_759532 (CHEMBL1811058) Inhibition of insulin receptor
- ChEMBL_794804 (CHEMBL1935987) Inhibition of insulin receptor
- ChEMBL_825876 (CHEMBL2044753) Inhibition of insulin receptor
- ChEMBL_90267 (CHEMBL699132) Inhibition of Insulin receptor
- ChEMBL_90276 (CHEMBL699141) Inhibition of Insulin receptor
- ChEBML_90279 Inhibition of Insulin receptor kinase-beta
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- ChEMBL_215892 (CHEMBL820824) Inhibition of beta-insulin receptor kinase
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- ChEBML_90397 Inhibition of Insulin-like growth factor I receptor
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- ChEMBL_2267608 Inhibition of Insulin receptor tyrosine kinase (unknown origin)
- ChEMBL_2297251 Binding affinity to insulin regulated aminopeptidase (unknown origin)
- ChEMBL_614233 (CHEMBL1106061) Inhibition of insulin receptor by HTRF assay
- ChEMBL_699678 (CHEMBL1648321) Inhibition of insulin receptor after 1 hr
- ChEMBL_885942 (CHEMBL2215704) Inhibition of insulin receptor by AlphaScreen analysis
- ChEMBL_90266 (CHEMBL699131) Inhibition of insulin receptor (InsR) tyrosine kinase
- ChEBML_90282 Inhibition of human insulin-like growth factor I receptor
- ChEMBL_305383 (CHEMBL832897) Inhibition of Insulin receptor kinase in P19 cells
- ChEMBL_566615 (CHEMBL960141) Inhibition of insulin receptor by virtual HTS assay
- ChEMBL_581979 (CHEMBL1058959) Inhibition of insulin receptor by cell based assay
- ChEMBL_88875 (CHEMBL698212) Activation of human insulin receptor tyrosine kinase (IRTK)
- ChEMBL_90285 (CHEMBL697504) Inhibition of Insulin-like growth factor I receptor
- ChEMBL_90396 (CHEMBL698351) Inhibition of Insulin-like growth factor I receptor
- ChEMBL_941897 (CHEMBL2329963) Inhibition of human recombinant IDE-mediated insulin degradation
- ChEBML_90404 Ability to displace Insulin-Like Growth Factor (IGF-I) from its binding to human insulin-like growth factor binding protein 3 (hIGFBP-3)
- ChEMBL_2527721 Inhibition of Insulin receptor expressed in HEK293 cells assessed as reduction insulin-stimulated INSR phosphorylation incubated for 1 hr by sandwich ELISA analysis
- ChEBML_90403 Ability of compound to displace Insulin-Like Growth Factor (IGF-I) from its binding to Insulin-like growth factor binding protein 3 (IGFBP-3)
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- ChEMBL_305115 (CHEMBL831583) Inhibition of human insulin-like growth factor I receptor
- ChEMBL_306046 (CHEMBL874552) Inhibition of human Insulin receptor expressed in CHO cells
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- ChEMBL_90265 (CHEMBL699130) Inhibition of insulin receptor mediated mitogenesis of NIH3T3 cells
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- ChEMBL_1869997 (CHEMBL4371164) Inhibition of human placental insulin receptor expressed in CHO cells assessed as decrease in insulin-stimulated [3H]-2-deoxyglucose uptake preincubated for 1 hr
- ChEMBL_950881 (CHEMBL2349705) Inhibition of Akt phosphorylation in human insulin-stimulated A549 cells incubated for 2 hrs prior to insulin-induction measured after 30 mins by ELISA
- ChEMBL_1767895 (CHEMBL4220007) Displacement of [TyrA14-125I]-human insulin from human insulin receptor isoform A expressed in baby hamster kidney cells after 2 days by gamma counting method
- ChEMBL_538724 (CHEMBL1035035) Activation of insulin receptor tyrosine kinase in mouse 3T3-L1 cells assessed as increase in 2-deoxy-D-[14C]glucose transport in presence of insulin
- ChEMBL_210560 (CHEMBL816512) Inhibition of thioredoxin reductase in the presence of thioredoxinand insulin
- ChEMBL_2377431 Non-covalent inhibition of PDI (unknown origin) by insulin aggregation assay
- ChEMBL_471122 (CHEMBL921275) Inhibition of human purified insulin receptor expressed in HepG2 cells
- ChEMBL_807032 (CHEMBL1959424) Inhibition of insulin receptor using fluorescent substrate by IMAP assay
- ChEMBL_90405 (CHEMBL698360) Inhibitory activity against Insulin-like growth factor binding protein 3
- ChEMBL_1706543 (CHEMBL4057776) Inhibition of insulin stimulated INSR phosphorylation in human HeLa cells preincubated for 1 hr followed by insulin addition measured after 5 mins by Western blot analysis
- ChEMBL_1570092 (CHEMBL3789694) Inhibition of insulin receptor (unknown origin) in presence of [gamma33P]ATP
- ChEMBL_519651 (CHEMBL946778) Inhibition of human insulin receptor autophosphorylation in transfected mouse NIH3T3 cells
- ChEMBL_591804 (CHEMBL1041544) Inhibition of insulin receptor by [gamma-33-P]ATP based assay
- ChEMBL_654586 (CHEMBL1243630) Inhibition of human insulin receptor-mediated Poly Glu4Tyr phosphorylation by ELISA
- ChEMBL_873671 (CHEMBL2188787) Agonist activity at rat P2Y1R assessed as glucose-dependent insulin secretion
- Reductase Activity Assay Reductase activity was assayed by measuring the PDI-catalyzed reduction of insulin in the presence of DTT, thus measuring the aggregation of reduced insulin chains at 650nm.
- ChEMBL_2567995 Inhibition of INSR phosphorylation in insulin-stimulated human H4-II-E cells preincubated with compound for 30 mins followed by insulin stimulation and measured after 10 mins by immunoblot analysis
- ChEMBL_1513260 (CHEMBL3610968) Inhibition of insulin receptor (unknown origin) by homogeneous time resolved fluorescence assay
- ChEMBL_745322 (CHEMBL1775397) Activation of FFA1 in mouse islets assessed as glucose-dependent insulin secretion
- ChEMBL_796984 (CHEMBL1944059) Inhibition of insulin receptor after 20 mins by time-resolved fluorescence assay
- ChEMBL_162259 (CHEMBL772438) Inhibitory activity against Protein-tyrosine phosphatase 1B-mediated dephosphorylation of phosphorylated insulin receptor using (CHO) cell line transfected with an expression plasmid encoding the normal human insulin receptor [CHO/HIRc]
- ChEMBL_2542048 Inhibition of human IR autophosphorylation in insulin- stimulated mouse NIH-3T3-hIR cells pre incubated for 6 hr followed by insulin stimulation and measured after 15 mins by Western blot analysis
- ChEMBL_197124 (CHEMBL801614) Effective concentration that reduces HIV-induced cytopathic effect by 50% was determined by reverse transcriptase (RT) assay.
- ChEMBL_162252 (CHEMBL770119) Inhibition of human Protein-tyrosine phosphatase 1B (PTP1B) dephosphorylation of insulin receptor peptide
- ChEMBL_521715 (CHEMBL1001626) Agonist activity at rat pancreas P2Y1 receptor assessed as enhancement of insulin secretion
- ChEMBL_801839 (CHEMBL1947451) Displacement of thioflavin T from insulin receptor by thioflavin-T fluorescent dye assay
- ChEMBL_90284 (CHEMBL697349) In vitro inhibition of Insulin-like growth factor I receptor expressed in baculovirus
- ChEMBL_1279808 (CHEMBL3095509) Activation of glucokinase in rat INS-1 cells assessed as glucose-stimulated insulin secretion
- ChEMBL_1672669 (CHEMBL4022698) Inhibition of human insulin receptor tyrosine kinase after 1 hr by scintillation counting method
- ChEMBL_2266110 Inhibition of Escherichia coil TrxR incubated for 2 hrs in presence of DTT and insulin
- ChEMBL_519642 (CHEMBL946769) Inhibition of GST-tagged insulin receptor expressed in baculovirus by time-resolved fluorescence assay
- ChEMBL_884453 (CHEMBL2212215) Inhibition of human recombinant TRX-2 up to 60 mins by insulin reduction assay
- ChEMBL_884454 (CHEMBL2212216) Inhibition of human recombinant TRX-1 up to 60 mins by insulin reduction assay
- ChEMBL_1909270 (CHEMBL4411716) Activation of insulin-stimulated glycogen synthase in human HepG2 cells using [U-14C]UDP glucose as substrate preincubated for 18 hrs followed by insulin stimulation and measured after 15 mins by beta-counting method
- ChEMBL_2545794 Inhibition of PI3Kbeta in human adipocytes assessed as reduction in insulin-induced 2-deoxy-[U-14C]-glucose uptake preincubated for 3 hrs followed by insulin addition and measured after 30 mins by microbeta scintillation counting analysis
- ChEMBL_800636 (CHEMBL1947668) Activation of SUR1 in rat pancreatic islets assessed as inhibition of glucose-induced insulin secretion
- ChEMBL_90401 (CHEMBL698356) The compound was tested for binding affinity against insulin-like growth factor binding protein 1
- ChEMBL_90402 (CHEMBL698357) The compound was tested for binding affinity against insulin-like growth factor binding protein 2
- ChEMBL_90406 (CHEMBL698361) The compound was tested for binding affinity against Insulin-like growth factor binding protein 4
- ChEMBL_90407 (CHEMBL698362) The compound was tested for binding affinity against Insulin-like growth factor binding protein 4
- ChEMBL_90544 (CHEMBL700614) The compound was tested for binding affinity against Insulin-like growth factor binding protein 5
- ChEMBL_90545 (CHEMBL700615) The compound was tested for binding affinity against Insulin-like growth factor binding protein 6
- ChEMBL_959585 (CHEMBL2382530) Agonist activity at GPR40 in rat INS-1 cells assessed as glucose-stimulated insulin secretion
- ChEMBL_776271 (CHEMBL1914068) Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Thr308 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
- ChEMBL_776272 (CHEMBL1914069) Inhibition of PIK3CA-mediated cell signaling in PTEN-deficient human U87MG cells assessed as inhibition of insulin-induced pAkt/PKB phosphorylation at Ser473 treated for 15 mins before insulin challenge measured after 5 mins by immunoblotting
- ChEMBL_197125 (CHEMBL803726) Reverse transcriptase activity was measured in the culture supernatant, concentration that reduces by 50% the HIV produced in the supernatant.
- ChEMBL_1719739 (CHEMBL4134739) Inhibition of TrxR1 in human HL60 cells incubated for 24 hrs by endpoint insulin reduction assay
- ChEMBL_858381 (CHEMBL2168596) Activation of glucokinase in rat INS-1 cells assessed as stimulation of glucose-induced insulin secretion
- ChEMBL_90408 (CHEMBL698363) Dissociation constant binding to Insulin-like growth factor binding protein 5 at the residue L-81
- ChEMBL_90424 (CHEMBL698181) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue L73
- ChEMBL_90425 (CHEMBL698182) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue L81
- ChEMBL_90426 (CHEMBL697415) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue R87
- ChEMBL_90427 (CHEMBL697416) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue S85
- ChEMBL_90428 (CHEMBL697417) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue Y50
- ChEMBL_90429 (CHEMBL697418) Dissociation constant in binding to Insulin-like growth factor binding protein 5 at the residue Y86
- ChEMBL_1570094 (CHEMBL3789696) Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation
- ChEMBL_1667905 (CHEMBL4017793) Inhibition of insulin receptor kinase (unknown origin) using TK as substrate after 30 mins by HTRF assay
- ChEMBL_1897038 (CHEMBL4399073) Inhibition of human recombinant IDE expressed in CHO cells in presence of [125I]-insulin by HTRF assay
- ChEMBL_581975 (CHEMBL1058955) Inhibition of insulin receptor-mediated proliferation of mouse NIH/3T3 cells after 48 hrs by MTT assay
- ChEMBL_90281 (CHEMBL697346) Concentration required to achieve 50% inhibition of tyrosine phosphorylation on human Insulin-like growth factor I receptor
- ChEMBL_90409 (CHEMBL698364) Dissociation constant in BS binding to Insulin-like growth factor binding protein 5 at the residue K91
- ChEMBL_90410 (CHEMBL698365) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue K91
- ChEMBL_90411 (CHEMBL698366) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue L73
- ChEMBL_90412 (CHEMBL698367) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue L81
- ChEMBL_90413 (CHEMBL698368) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue R87
- ChEMBL_90414 (CHEMBL698369) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue S85
- ChEMBL_90415 (CHEMBL698218) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue Y50
- ChEMBL_90416 (CHEMBL698219) Dissociation constant in DMSO binding to Insulin-like growth factor binding protein 5 at the residue Y86
- ChEMBL_90417 (CHEMBL698220) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue K91
- ChEMBL_90418 (CHEMBL698221) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue L73
- ChEMBL_90419 (CHEMBL698222) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue L81
- ChEMBL_90420 (CHEMBL698223) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue R87
- ChEMBL_90421 (CHEMBL698838) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue S85
- ChEMBL_90422 (CHEMBL698839) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue Y50
- ChEMBL_90423 (CHEMBL698180) Dissociation constant in PBS binding to Insulin-like growth factor binding protein 5 at the residue Y86
- ChEMBL_631420 (CHEMBL1111957) Inhibition of insulin receptor assessed as [33P]gamma-ATP incorporation into substrate after 60 mins by gamma counting
- ChEMBL_1339905 (CHEMBL3243742) Induction of human recombinant IDE-mediated insulin hydrolysis preincubated for 10 mins measured after 30 mins by spectrophotometer analysis
- ChEMBL_2524990 Inhibition of GST-tagged human Insulin receptor expressed in baculovirus infected Sf9 cells using retinoblastoma protein in presence of ATP
- ChEMBL_675743 (CHEMBL1272377) Inhibition of Pin1 in serum starved human PC3 cells assessed as reduction in insulin-induced p7)S6 kinase phosphorylation
- ChEMBL_1869996 (CHEMBL4371163) Non-competitive inhibition of human placental insulin receptor expressed in CHO cell membrane assessed as decrease in insulin-stimulated A2 phosphorylation preincubated for 15 mins followed by substrate addition and measured after 15 mins in presence of [gamma-32P]ATP by Dixon plot analysis
- ChEMBL_1455264 (CHEMBL3362270) Agonist activity at mouse FFA4 receptor in mouse MIN6 cells assessed as induction of glucose-induced insulin secretion by AlphaLISA
- ChEMBL_1565351 (CHEMBL3782745) Inhibition of human recombinant PTP-1B using IR5 insulin receptor residues as substrate after 30 mins by malachite green assay
- ChEMBL_1623252 (CHEMBL3865604) Agonist activity at GPR40 in rat RINm cells assessed as increase glucose-stimulated insulin secretion after 1 hr by ELISA
- ChEMBL_1850470 (CHEMBL4351094) Inhibition of PI3Kdelta (unknown origin) preincubated for 30 mins followed by insulin stimulation for 5 mins by Western blot analysis
- ChEMBL_1922001 (CHEMBL4424846) Inhibition of human N-terminal His6-tagged insulin receptor (1005 to 1310 residues) expressed in baculovirus infected Sf21 insect cells
- ChEMBL_1775688 (CHEMBL4232680) Inhibition of human IDE using insulin as substrate preincubated for 10 mis followed by substrate addition and measured after 30 mins
- ChEMBL_1883833 (CHEMBL4385332) Agonist activity at GPR40 in human islets assessed as induction of glucose-stimulated insulin secretion after 1 hr by HTRF assay
- ChEMBL_2028620 (CHEMBL4682778) Inhibition of PDIA3 (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr and measured by insulin reduction assay
- ChEMBL_2028621 (CHEMBL4682779) Inhibition of PDIA4 (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr and measured by insulin reduction assay
- ChEMBL_2028623 (CHEMBL4682781) Inhibition of PDIA6 (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr and measured by insulin reduction assay
- ChEBML_1645791 Agonist activity at GLP1R in rat INS-1 cells assessed as increase in glucose-stimulated insulin secretion after 1 hr by HTRF assay
- ChEMBL_1897041 (CHEMBL4399076) Inhibition of recombinant IDE exosite (unknown origin) expressed in Escherichia coli using insulin as substrate incubated for 4 hrs by AlphaLisa assay
- ChEMBL_1296283 (CHEMBL3132611) Inhibition of Insulin receptor (unknown origin) using biotinylated poly-Glu-Tyr (4:1) as substrate preincubated for 5 mins measured after 12 hrs
- ChEMBL_1645791 (CHEMBL3994847) Agonist activity at GLP1R in rat INS-1 cells assessed as increase in glucose-stimulated insulin secretion after 1 hr by HTRF assay
- ChEMBL_1861481 (CHEMBL4362337) Inhibition of TrxR1 (unknown origin) using DTNB as substrate preincubated for 30 mins in presence of insulin followed by substrate addition by colorimetry
- ChEMBL_2069558 (CHEMBL4724811) Agonist activity at GPR119 in glucose-induced golden hamster HIT-T15 cells assessed as increase in insulin secretion after 2 hrs by A1phaLISA
- ChEMBL_971485 (CHEMBL2406363) Inhibition of TEL-fused insulin receptor (unknown origin) expressed in mouse BAF3 cells after 2 to 3 days by luciferase reporter gene assay
- ChEMBL_1784836 (CHEMBL4256353) Inhibition of NADPH-reduced recombinant rat TrxR1 expressed in Escherichia coli harboring gor mutant assessed as suppression of insulin reduction using Trx as substrate pretreated for 30 mins followed by Trx addition for 30 mins and subsequent eosin-labelled bovine insulin addition measured every 5 mins for 1 hr by fluorescence assay
- ChEMBL_2104460 (CHEMBL4812963) Agonist activity at rat GPR119 in golden hamster HIT-T15 cells assessed as induction of glucose-induced insulin secretion after 2 hrs by A1phaLISA
- ChEMBL_1661563 (CHEMBL4011175) Induction of ERalpha degradation in human MCF7 cells assessed as inhibition of insulin-mediated cell proliferation after 6 days by Hoechst 33258 dye-based assay
- ChEMBL_1888984 (CHEMBL4390738) Inhibition of recombinant human N-terminal His-tagged PDI expressed in Escherichia coli BL21 (DE3) pLysS assessed as reduction in enzyme-mediated bovine insulin aggregation
- ChEMBL_863868 (CHEMBL2176258) Inhibition of INSR expressed in CHO cells assessed as inhibition of receptor phosphorylation pre-incubated before insulin stimulation by Meso-Scale Discovery pY-IR assay
- ChEMBL_218251 (CHEMBL819219) In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle
- ChEMBL_1933011 (CHEMBL4478663) Inhibition of AKT1 phosphorylation at Ser473 in EGF/insulin-stimulated human AN3CA cells incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_1933012 (CHEMBL4478664) Inhibition of AKT1 phosphorylation at Ser473 in EGF/insulin-stimulated human A2780 cells incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_1933013 (CHEMBL4478665) Inhibition of AKT1 phosphorylation at Thr308 in EGF/insulin-stimulated human AN3CA cells incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_1933014 (CHEMBL4478666) Inhibition of AKT1 phosphorylation at Thr308 in EGF/insulin-stimulated human A2780 cells incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_1897052 (CHEMBL4399087) Inhibition of wild type human IDE catalytic site using insulin as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by Luminex kit method
- ChEMBL_1988385 (CHEMBL4621932) Inhibition of PI3Kalpha in human BT474 cells expressing P3KCA mutant assessed as reduction in AKT phosphorylation at residue S473 incubated for 2 hrs followed by insulin addition by ELISA
- Metabolic Measurements Glucose in tail blood was measured using a glucometer (One-Touch Basic; Lifescan, CA). For glucose tolerance tests (GTTs), mice were fasted for 10 hours and then injected with 20% D-glucose (2 mg/g body weight) and the blood glucose was monitored immediately before and at 15, 30, 60 and 120 mins following the injection. For insulin tolerance tests (ITTs), 4-h fasted animals were given insulin (0.75 mU/g) and blood glucose was measured immediately before and at 30, 60 and 120 minutes postinjection. Serum insulin, cholesterol, triglycerides (Stanbio Labs, TX), BDNF (Abnova), IGF1 and IGFBPs (R&D Systems) were determined by enzyme-linked immunosorbent assay.
- ChEMBL_1570093 (CHEMBL3789695) Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis
- ChEMBL_1933015 (CHEMBL4478667) Inhibition of AKT1 in EGF/insulin-stimulated human AN3CA cells assessed as reduction in phosphorylation at Thr246 incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_1933016 (CHEMBL4478668) Inhibition of AKT1 in EGF/insulin-stimulated human A2780 cells assessed as reduction in phosphorylation at Thr246 incubated for 1 hr followed by stimulation for 15 mins by Western blot analysis
- ChEMBL_2074276 (CHEMBL4729810) Inhibition of recombinant human wild-type N-terminal His-tagged PDIA1 expressed in Escherichia coli strain BL21(DE3) using bovine insulin as substrate preincubated for 1 hr followed by substrate addition
- ChEMBL_2516987 Inhibition of Ins-R in A14 [Human melanoma] cells assessed as inhibition of autophosphorylation of Ins-R incubated for 90 mins followed by insulin stimulation measured after 10 mins by ELISA analysis
- ChEMBL_901085 (CHEMBL3062690) Agonist activity at Homo sapiens (human) PPARgamma expressed in mouse 3T3-L1 cells incubated for 2 days followed by compound wash out measured after 4 days by insulin receptor binding assay
- ChEMBL_1767894 (CHEMBL4220006) Agonist activity at B6D2F1 mouse insulin receptor assessed as increase in glucose incorporation into lipid phase after 2 hrs in presence of D-[3-3H]glucose by TopCount microplate scintillation counting method
- ChEMBL_1897053 (CHEMBL4399088) Inhibition of human recombinant IDE expressed in Escherichia coli BL21 (DE3) cells using insulin as substrate preincubated for 10 mins followed by substrate addition and measured after 15 mins by fluorescence based assay
- ChEMBL_2264503 Inhibition of GST-tagged recombinant human IR ( 919 to 1343 residues) autophosphorylation expressed in mouse NIH-3T3-A14 cells preincubated for 90 mins followed by insulin stimulation and measured after 10 mins by ELISA
- ChEMBL_2248960 (CHEMBL5163170) Positive allosteric modulator activity at GLP-1R in rat INS1 beta-cells assessed potentiation of GLP-1(7-36)NH2 induced insulin secretion incubated for 30 mins in presence of high glucose condition by ELISA
- ChEMBL_1717891 (CHEMBL4132891) Antagonist activity at GLUT4 in rat adipocytes assessed as reduction in insulin-stimulated [3H]2-deoxyglucose uptake preincubated for 1 min followed by [3H]2-deoxyglucose addition measured after 1 min by liquid scintillation counting analysis
- ChEMBL_2248961 (CHEMBL5163171) Positive allosteric modulator activity at GLP-1R in rat INS1 beta-cells assessed potentiation of GLP-1(7-36)NH2 induced insulin secretion incubated for 30 mins in presence of 0.2 nM of GLP-1 by ELISA
- ChEMBL_2248962 (CHEMBL5163172) Positive allosteric modulator activity at GLP-1R in rat INS1 beta-cells assessed potentiation of GLP-1(7-36)NH2 induced insulin secretion at 0.1 nM incubated for 30 mins in presence of exendin(9-39)NH2 by ELISA
- ChEMBL_1661323 (CHEMBL4010935) Agonist activity at TGR5 in STC1 cells derived from double transgenic mouse expressing rat insulin promoters linked to SV40 large T antigen and to polyomavirus small T antigen assessed as increase in cAMP level after 40 mins by mass spectrometric method
- ChEMBL_662256 (CHEMBL1252348) Inhibition of PKB/Akt activation in human overnight starved MCF7 cells assessed as phosphorylated Akt at Ser473 level at 50 ug/ml after 1 hr followed by treated with 1 ug/mL of insulin for 15 mins by Western blotting
- Fluorescent Assay ABHD6: Certain compounds were tested for their ABHD6 and dual ABHD6/MGL inhibitory activity, which is expressed as % of inhibition or IC50 values. The percentage of inhibition describes the percentage by which the inhibitor reduces the velocity/rate of 2-AG hydrolysis by ABHD6, and MGL or AEA hydrolysis by FAAH.
- Intracellular ZAP-70 Kinase Inhibition Assay A coupled spectrophotometric assay was used wherein ADP generated by ZAP-70 kinase was converted to ATP by pyruvate kinase (PK), with concomitant production of pyruvate from phosphoenolpyruvate (PEP). LDH reduces pyruvate to lactate by oxidizing NADH. NADH depletion was monitored at 340 nm using a microplate reader (Spectra Max 250, Molecular Device).
- Kinase Inhibition Assay Compounds were evaluated for their ability to prevent phosphorylation of a model glutamate-tyrosine copolymer substrate by isolated human FGFR-1, mouse PDGF-beta receptor (PDGFR), or avian c-Src tyrosine kinase (all full length enzymes). IC50 is defined as the concentration of inhibitor that reduces by 50% the level of gamma-32P incorporated into the copolymer substrate.
- cAMP Assays Activation of GLP-1 receptor is known to stimulate cyclic AMP (cAMP) production in cells which indicates primary coupling to the G as subunit of the G protein heterotrimeric complex. Evidence suggests signaling through G as induced cAMP stimulation elicits the desired pharmacological response regarding insulin release from pancreatic β-cells.
- Ki Determination A coupled spectrophotometric assay was used in which ADP generated by kinase was converted to ATP with the concomitant production of pyruvate from PEP. LDH reduces pyruvate to lactate with the oxidation of NADH. NADH depletion was monitored at 340 nm using a microplate reader. The IC50 was evaluated from the data as a function of inhibitor concentration. The Ki value was calculated according to the Cheng-Prusoff approximation.
- Inhibition of ALK IR Anaplastic Lymphoma Kinase Activity To measure the activity of the N2-(2-methoxyphenyl)pyrimidine derivative represented by formula 1 of the present invention to inhibit anaplastic lymphoma kinase (ALK) activity at enzyme level, the following experiment was performed by the same manner as described in experimental example 1 except that IR (Insulin Receptor) protein was used instead of ALK WT protein.
- Enzyme Inhibition Assay A coupled spectrophotometric assay was used in which ADP generated by ERK2 was converted to ATP by pyruvate kinase with the production of pyruvate from phosphoenol pyruvate. Lactate dehydrogenase reduces pyruvate to lactate with the oxidation of NADH. NADH depletion was monitored at 340 nm using a microplate reader. The decrease of absorbance was monitored as a function of time and the resulting data was fitted to a competitive inhibition kinetic model to determine the Ki.
- In vitro Assay The method of determining thioredoxin activity is based on the reduction of insulin by thioredoxin. Thioredoxin is reconstituted is by thioredoxin reductase, with NADPH. The resulting free thiol -SH groups react with 5,5′-dithiobis-2-nitrobenzoic acid (DTNB). The termination of the reaction results in the formation of a red colour. The intensity of colouration is determined spectrophotometrically at 412 nm and this corresponds to the number of reduced sulfahydryl groups. The reaction was performed at 37° C. over 30 min. in a buffer containing 50 mM Tris-HCl and 20 mM EDTA at a pH of 7.6. The substrate concentrations used were: 0.25 μM human recombinant thioredoxin and 0.325 μM rat recombinant thioredoxin reductase (IMCO Corporation Ltd AB, Sweden) and 316 μM of insulin, 0.8 μM NADPH, 8 mM DTNB (Sigma Aldrich).
- Binding Assay The test was carried out as in 1, with the following modifications: cytosol from androgen receptor-expressing insect cells (Hi5) was used, and the reference substance was 3H-testosterone.The results of the binding tests and the ratio of the competition factors CF(PR) and CR(MR) are shown in Table 1, which for comparison also shows receptor binding values of drospirenone as reference substance A.
- Binding Assay The test was carried out as in 1., with the following modifications: cytosol from androgen receptor-expressing insect cells (Hi5) was used, and the reference substance was 3H-testosterone.The results of the binding tests and the ratio of the competition factors CF(PR) and CR(MR) are shown in Table 1, which for comparison also shows receptor binding values of drospirenone as reference substance A.
- Dose Response: Fluorescence polarization-based cell-based high throughput dose response assay for inhibitors of insulin-degrading enzyme (IDE) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Malcolm Leissring, Mayo Clinic College of Medicine Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 DA024888-01 Grant Proposal PI: Malcolm Leissring, Mayo Clinic College of Medicine External Assay ID: IDE_INH_FP_1536_3XIC50 DRUN Name: Dose Response: Fluorescence polarization-based cell-based high throughput dose response assay for inhibitors of insulin-degrading enzyme (IDE). Description: Alzheimer's disease (AD) is characterized by accumulation of amyloid beta-protein (A-beta; Abeta) in brain regions involved in memory and cognition (1). The steady-state levels of AB reflect a balance between its production via beta- and gamma-secretases and its catabolism by proteolytic degradation (2-4). Because Abeta cleavage products are less neurotoxic than intact Abeta, e
- PDI Inhibition Assay The assay was carried out in 384-well plates according to literature procedures [46]. Each well contained 100mM sodium phosphate and 0.2mM EDTA pH 7.0. 10ng PDI was pre-incubated with various concentration of probes (4% DMSO) in 20uL buffer for 30 min at 37 degrees Celsius, followed by the addition of insulin (0.16mM final concentration) and DDT (1mM final concentration). The enzyme reaction was monitored at 650nm on a Bioteck microplate reader.
- CA Enzyme Assay CA activity was measured by the Maren method that is based on determination of the time required for the pH to decrease from 10.0 to 7.4 due to CO2 hydration. Phenolred was added to the assay medium as the pH indicator, and the buffer was 0.5 M Na2CO3/0.1 M NaHCO3 (pH 10.0). One unit of CA activity is defined as the amount ofthe enzyme that reduces by 50% the time of CO2 hydration measured in the absence of enzyme. In the inhibition studies, the CO2 concentration was 70 mM and at last five different inhibitor concentrations were used.
- Inhibition Assay Seven point five μL per well of human TrkA (PV3144, Lifetechnologies, final concentration: 1 nmol/L) suspended in the assay buffer (100 mmol/L 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES), 10 mmol/L magnecium chloride, 0.003 vol % Brij-35, 0.004 vol % Tween20 and 1 mmol/L dithiothreitol (DTT)) was applied in a 384 well plate and the plate was pre-incubated for 15 min at room temperature with 0.4 μL of each compound (final concentration: 200 μmol/L-1 pmol/L) dissolved in DMSO. Then, fluorescent substrate (FL-peptide 27, 760424, PerkinElmer, final concentration: 1.5 μmol/L) and ATP (final concentration 500 μmol/L) dissolved in the assay buffer was added in each well. After the incubation of 120 min at 37° C., fifteen μL of termination buffer (100 mmol/L HEPES, 40 mmol/L ethylenediaminetetraacetic acid (EDTA), 10 mmol/L magnecium chloride, 0.003 vol % Brij-35, 0.004 vol % Tween20, 1 mmol/L DTT and 0.16 vol % Coating Reagent 3) was added in each well to stop the enzyme reaction. Fluorescent intensities (FI) of phosphorylated and non-phosphorylated fluorescent substrates were measured by LabChip EZReader II (Caliper LifeSciences, Inc.), and conversion ratio (CR) was calculated by the following formula-1. The CR in the well applied with DMSO alone was used as a negative control and the CR in the well without applying TrkA was used as a positive control.