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17-cyclopropylmethyl-6,7-didehydro-4,5-epoxy-5'-guanidinyl-3,14-dihydroxyindolo(2',3'-6,7)morphinan (CID 9826034) - Compound BioActivity Data
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BioActivity Outcomes:
Active(50)
 
 
Inactive(42)
 
 
Inconclusive(16)
 
 
Unspecified(18)
 
 
Top Targets:
7TM GPCR Srsx(7)
 
 
 
 
7TM GPCR Srx(6)
 
 
 
PIKKc TOR(4)
 
 
 
Pyr redox dim(4)
 
 
 
Hexokinase 2(3)
 
 
BioAssay Types:
Confirmatory(66)
 
 
 
 
Literature(60)
 
 
 
 
 
BioActivity Types:
Potency(67)
 
 
 
 
Ki(25)
 
 
Kd(3)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 119    Data Row: 126   Total Pages: 3   Display: Page     
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#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103583410]
Ki 3e-05Displacement of [3H]diprenorphine from k-Y312A-receptor expressed in HEK 293 cells [AID148585, Type: Literature]
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2
[SID103583410]
Kd 3.98e-05Antagonistic activity against human cloned kOpioid receptor kappa 1 using U69,593 in [35S]GTP-gamma-S, assay [AID148169, Type: Literature]
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3
[SID103583410]
Ki 6e-05Mutant factor of the compound against mu-[K303E] with Opioid receptor kappa 1 for binding affinity [AID148599, Type: Literature]
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4
[SID103583410]
Ki 9e-05Displacement of [3H]- diprenorphine from mu-K303E-receptor expressed in HEK 293 cells [AID152386, Type: Literature]
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5
[SID103583410]
Ki 9e-05Effect on binding affinity of mutational exchange of Glu297 in the Opioid receptor kappa 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. [AID148588, Type: Literature]
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6
[SID103583410]
Ki 0.00014Binding affinity towards rat opioid receptor kappa 1 was determined using [3H]diprenorphine radioligand [AID148575, Type: Literature]
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7
[SID103583410]
Ki 0.00015Displacement of [125I]-IBNtxA from KOR-1 expressed in CHO cells [AID603174, Type: Literature]
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8
[SID103583410]
Ki 0.00018Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells [AID148586, Type: Literature]
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9
[SID103583410]
Ki 0.00018Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor kappa 1 [AID148568, Type: Literature]
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10
[SID103583410]
Ki 0.00018Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of guinea pig brain [AID149260, Type: Literature]Kappa-type opioid receptor [gi:730228]
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11
[SID103583410]
Ki 0.00019Displacement of [125I]-IBNalA from KOR-1 expressed in CHO cells [AID603175, Type: Literature]
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12
[SID103583410]
Ki 0.00021Effect on binding to wild-type opioid receptor kappa 1 using [3H]diprenorphine in transiently expressed rat HEK293 cells [AID148590, Type: Literature]
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13
[SID103583410]
Ki 0.0005Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells [AID152388, Type: Literature]
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14
[SID103583410]
Ki 0.0011Displacement of [3H]- diprenorphine from delta-W284E-receptor expressed in HEK 293 cells [AID149086, Type: Literature]
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15
[SID103583410]
Kd 0.00324Antagonistic activity against human cloned Opioid receptor mu 1 using DPDPE in [35S]GTP-gamma-S, assay [AID151116, Type: Literature]
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16
[SID103583410]
Ki 0.0039Displacement of [3H]diprenorphine from k-E297A-receptor expressed in HEK 293 cells [AID148584, Type: Literature]
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17
[SID103583410]
Ki 0.00393Effect on binding to kappa(Glu297Ala) opioid receptor, using [3H]diprenorphine in transiently expressed rat HEK293 cells [AID148589, Type: Literature]
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18
[SID103583410]
Ki 0.00923Effect on binding affinity of mutational exchange of Lys303 in the Opioid receptor mu 1 in transiently expressed rat cos-7 cells activity expressed as binding affinity. [AID151766, Type: Literature]
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19
[SID103583410]
Ki 0.0129Mutant factor of the compound against kappa[E297K] with Opioid receptor kappa 1 for binding affinity. [AID148598, Type: Literature]
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20
[SID103583410]
Kd 0.01549Antagonistic activity against human cloned Opioid receptor delta 1 using DPDPE in [35S]GTP-gamma-S, assay [AID148383, Type: Literature]
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21
[SID103583410]
Ki 0.0225Displacement of [3H]- diprenorphine from mu-receptor expressed in HEK 293 cells [AID152389, Type: Literature]
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22
[SID103583410]
Ki 0.0225Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor mu 1 [AID151614, Type: Literature]
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23
[SID103583410]
Ki 0.0248Binding affinity towards mouse delta-opioid receptor was determined using [3H]diprenorphine as radioligand [AID149248, Type: Literature]
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24
[SID103583410]
Ki 0.0369Inhibition of [3H]DAMGO binding to Opioid receptor mu 1 of rat brain tissue [AID151620, Type: Literature]Mu-type opioid receptor [gi:464314]
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25
[SID103583410]
Ki 0.0462Binding affinity on HEK293 cells transiently transfected with plasmids encoding the rat Opioid receptor delta 1 [AID149675, Type: Literature]
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26
[SID103583410]
Ki 0.0462Displacement of [3H]- diprenorphine from delta receptor expressed in HEK 293 cells [AID149085, Type: Literature]
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27
[SID103583410]
Ki 0.07Inhibition of [3H]-DADLE binding to Opioid receptor delta 1 of rat brain tissue [AID149783, Type: Literature]Delta-type opioid receptor [gi:464311]
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28
[SID103583410]
Ki 0.0997Binding affinity towards rat mu-opioid receptor was determined using [3H]diprenorphine as radioligand [AID152373, Type: Literature]
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29
[SID90341628]
Potency 1.2589qHTS Assay for Inhibitors of Histone Lysine Methyltransferase G9a [AID504332, Type: confirmatory]euchromatic histone-lysine N-methyltransferase 2 [Homo sapiens] [gi:168985070]
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30
[SID90341628]
Potency 2.1192qHTS Validation Assay for Inhibitors for MPP8 Chromodomain Interactions with Methylated Histone Tails [AID488949, Type: confirmatory]M-phase phosphoprotein 8 [Homo sapiens] [gi:41055989]
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31
[SID90341628]
Potency 2.31qHTS for Inhibitors of binding or entry into cells for Lassa Virus [AID540256, Type: confirmatory]
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32
[SID90341628]
Potency 2.9093qHTS of Nrf2 Activators: LOPAC Validation [AID624149, Type: confirmatory]Nrf2 [Homo sapiens] [gi:693842]
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33
[SID90341628]
Potency 3.5481qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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34
[SID90341628]
Potency 23.7781Inhibitors of Regulator of G Protein Signaling (RGS) 4: qHTS [AID504845, Type: confirmatory]regulator of G-protein signaling 4 [Homo sapiens] [gi:86301163]
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35
[SID90341628]
Potency 25.9185qHTS for inhibitors of binding or entry into cells for Marburg Virus [AID540276, Type: confirmatory]gene 4 small orf - Marburg virus [gi:420597]
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36
[SID50111078]
Potency 25.9185qHTS for inhibitors of binding or entry into cells for Marburg Virus [AID540276, Type: confirmatory]gene 4 small orf - Marburg virus [gi:420597]
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37
[SID90341628]
Potency 26.6795qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1): qHTS [AID588453, Type: confirmatory]thioredoxin reductase [Rattus norvegicus] [gi:8659577]
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38
[SID90341628]
Potency 26.6795qHTS Assay for Inhibitors of Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1) [AID488773, Type: confirmatory]thioredoxin reductase [Rattus norvegicus] [gi:8659577]
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39
[SID90341628]
Potency 28.1838qHTS Validation Assay for Inhibitors of HP1-beta Chromodomain Interactions with Methylated Histone Tails [AID488953, Type: confirmatory]chromobox protein homolog 1 [Homo sapiens] [gi:187960037]
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40
[SID90341628]
Potency 35.4813Inhibitors of the vitamin D receptor (VDR): qHTS [AID504847, Type: confirmatory]vitamin D3 receptor isoform VDRA [Homo sapiens] [gi:63054845]
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41
[SID90341628]
Potency 79.4328Inhibitors of USP1/UAF1: Pilot qHTS [AID504865, Type: confirmatory]USP1 protein [Homo sapiens] [gi:118600387]
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42
[SID103583410]
Opioid antagonist potencies against Opioid receptor mu 1 from guinea pig ileum employing morphine(M) as agonist. [AID147887, Type: Literature]Mu-type opioid receptor [gi:3024265]
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43
[SID103583410]
Opioid receptor mu 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) [AID147889, Type: Literature]Mu-type opioid receptor [gi:3024265]
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44
[SID103583410]
Opioid antagonist potency, determined in guinea pig ileum (GPI) preparation, using morphine (mu-opioid) as agonist (Ke=antagonist/IC50 ratio -1) [AID152223, Type: Literature]Mu-type opioid receptor [gi:3024265]
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45
[SID103583410]
Inhibition of U50488-induced analgesic activity against C57BL/6 mouse assessed as tail withdrawal latecy at 10 mg/kg, ip upto 21 days [AID381420, Type: Literature]
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46
[SID103583410]
Opioid antagonist potencies against Opioid receptor kappa 1 from guinea pig ileum employing ethylketazocine (EKC) as agonist. [AID148972, Type: Literature]Kappa-type opioid receptor [gi:730228]
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47
[SID103583410]
Opioid antagonist potency towards opioid receptor kappa 1 determined in guinea pig ileum preparation [AID148973, Type: Literature]Kappa-type opioid receptor [gi:730228]
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48
[SID103583410]
Opioid receptor kappa 1 Antagonism (100 nM) is expressed as (Ke = [antagonist] / (IC50 ratio -1) [AID148975, Type: Literature]Kappa-type opioid receptor [gi:730228]
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49
[SID103583410]
Opioid antagonist potencies against Opioid receptor delta 1 from mouse vas-deferens preparation employing [D-Ala2,D-Leu5]enkephalin (DADLE) as agonist. [AID148938, Type: Literature]
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50
[SID103583410]
Opioid antagonist potency, determined in mouse vas deferens (MVD) preparation, using DADLE (delta-opioid) as agonist (Ke=antagonist/IC50 ratio -1) [AID148939, Type: Literature]
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