Nitrendipine (CID 4507) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(75)
 
 
Inactive(1155)
 
 
Inconclusive(120)
 
 
Unspecified(222)
 
 
Top Targets:
7TM GPCR Srx(46)
 
 
 
 
7TM GPCR Srsx(25)
 
 
 
Bcl-2 like(20)
 
 
alkPPc(20)
 
 
Tryp SPc(15)
 
 
 
BioAssay Types:
Screening(644)
 
 
 
 
Confirmatory(521)
 
 
 
 
 
Literature(225)
 
 
 
 
 
Summary(1)
 
 
BioActivity Types:
Potency(418)
 
 
 
 
 
IC50(224)
 
 
 
 
 
EC50(22)
 
 
 
 
Ki(5)
 
 
 
Kd(4)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1136    Data Row: 1572   Total Pages: 32   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103589735]
IC50 0.00015Inhibition of [3H]nitrendipine binding to L-type calcium channel of guinea pig ileal longitudinal smooth muscle [AID45611, Type: Literature]
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2
[SID103589735]
Ki 0.00025Inhibition of [3H]nitrendipine binding to L-type calcium channel dihydropyridine site of porcine cardiac sarcolemma membrane vesicles [AID56027, Type: Literature]
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3
[SID103589735]
Kd 0.00026Dissociation constant for high affinity binding sites in intact cultured cardiac cells [AID27147, Type: Literature]
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4
[SID103589735]
Kd 0.00026Inhibition of [3H]nitrendipine binding to L-type calcium channel in guinea pig ventricular myocardium membranes [AID45616, Type: Literature]
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5
[SID103589735]
IC50 0.000383DRUGMATRIX: Calcium Channel Type L, Dihydropyridine radioligand binding (ligand: [3H] Nitrendipine) [AID625216, Type: other]
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6
[SID103589735]
IC50 0.001In vitro vasorelaxant activity (calcium channel blocking activity) was determined with potassium-depolarized rabbit thoracic aorta [AID45769, Type: Literature]
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7
[SID103589735]
IC50 0.001Vasorelaxant potency in isolated potassium (K(+)-depolarized rabbit thoracic aorta. [AID167810, Type: Literature]
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8
[SID103589735]
IC50 0.0013Inhibition of rat L-type Ca2+ channel dihydropyridine site [AID566278, Type: Literature]
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9
[SID103589735]
IC50 0.00157DRUGMATRIX: Calcium Channel Type L, Benzothiazepine radioligand binding (ligand: [3H] Diltiazem) [AID625215, Type: other]
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10
[SID103589735]
IC50 0.003Inhibition of human voltage-dependent L-type calcium channel subunit alpha1C/alpha2delta/beta2a expressed in C1-6-37-3 cells assessed as inhibition of K+-induced calcium influx incubated for 30 mins prior to K+-induction by Fluo-4-AM based FLIPR assay [AID674363, Type: Literature]
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11
[SID103589735]
IC50 0.0031Dose-dependent inhibition of calcium contraction in depolarized rat aortic strips [AID179416, Type: Literature]
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12
[SID103589735]
IC50 0.01Ability to block depolarization induced 45Ca uptake into pheochromocytoma PC12 cells [AID156513, Type: Literature]
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13
[SID103589735]
Kd 0.01Dissociation constant for binding to isolated membranes from clonal cell line [AID27146, Type: Literature]
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14
[SID103589735]
Kd 0.016Dissociation constant for low affinity binding sites in intact cultured cardiac cells [AID27148, Type: Literature]
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15
[SID103589735]
IC50 0.016The compound was tested for inhibition of calcium influx into neuronal (NG108-15) cells [AID146413, Type: Literature]
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16
[SID103589735]
EC50 0.028Effective concentration for negative inotropic effect [AID175664, Type: Literature]
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17
[SID103589735]
EC50 0.03Vasorelaxant activity in Wistar rat endothelium-denuded thoracic aortic ring assessed as inhibition of noradrenaline-induced contraction treated after noradrenaline challenge measured after 60 mins [AID488212, Type: Literature]
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18
[SID103589735]
ID50 0.2[Ca2+] antagonistic activity on [Ca2+] current in guinea pig single ventricular cells [AID76668, Type: Literature]
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19
[SID103589735]
IC50 0.3DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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20
[SID103589735]
IC50 0.3DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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21
[SID103589735]
IC50 0.3DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625248, Type: other]Cytochrome P450 2C9 [gi:6686268]
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22
[SID855994]
IC50 1.46521Image-Based HTS for Selective Antagonists for GPR55 [AID2013, Type: confirmatory]G-protein coupled receptor 55 [Homo sapiens] [gi:33695107]
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23
[SID50104488]
Potency 2.5119qHTS 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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24
[SID103589735]
IC50 3DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625247, Type: other]Cytochrome P450 2C19 [gi:60416369]
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25
[SID103589735]
IC50 3DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) [AID625247, Type: other]Cytochrome P450 2C19 [gi:60416369]
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26
[SID103589735]
EC50 3.8Agonist activity at mouse TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium influx [AID482149, Type: Literature]Transient receptor potential cation channel subfamily A member 1 [gi:56749781]
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27
[SID855994]
Potency 5.8584Primary qHTS for delayed death inhibitors of the malarial parasite plastid, 48 hour incubation [AID504832, Type: confirmatory]
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28
[SID50104488]
Potency 6.3096qHTS for differential inhibitors of proliferation of Plasmodium falciparum line W2 [AID1883, Type: confirmatory]
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29
[SID103589735]
IC50 7.94328Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay [AID524790, Type: Literature]
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30
[SID103589735]
IC50 7.94328Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay [AID524796, Type: Literature]
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31
[SID103589735]
Ki 8.3Displacement of [125]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells [AID34564, Type: Literature]
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32
[SID50104488]
Potency 8.9125qHTS for differential inhibitors of proliferation of Plasmodium falciparum line 3D7 [AID1876, Type: confirmatory]
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33
[SID103589735]
Ki 8.96Displacement of [3H](R)-PIA binding to Adenosine A1 receptor in rat brain membranes [AID31706, Type: Literature]
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34
[SID90341570]
Potency 9.2qHTS Validation Assay to Find Inhibitors of Chronic Active B-Cell Receptor Signaling [AID485345, Type: confirmatory]
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35
[SID103589735]
IC50 10Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay [AID524791, Type: Literature]
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36
[SID103589735]
IC50 10Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay [AID524793, Type: Literature]
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37
[SID103589735]
IC50 10Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay [AID524795, Type: Literature]
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38
[SID103589735]
IC50 10Inhibitory concentration against potassium channel HERG [AID243151, Type: Literature]
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39
[SID103589735]
IC50 10Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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40
[SID103589735]
IC50 10Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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41
[SID103589735]
IC50 10Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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42
[SID103589735]
IC50 10Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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43
[SID103589735]
IC50 10Inhibition of human Potassium channel HERG expressed in mammalian cells [AID161281, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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44
[SID103589735]
IC50 10Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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45
[SID103589735]
IC50 10Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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46
[SID103589735]
IC50 10Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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47
[SID103589735]
IC50 10Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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48
[SID103589735]
IC50 10Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique [AID408340, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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49
[SID103589735]
IC50 10Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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50
[SID103589735]
IC50 10Inhibition of human ERG [AID576612, Type: Literature]Potassium voltage-gated channel subfamily H member 2 [gi:7531135]
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