ramatroban (CID 123879) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(33)
 
 
Inactive(90)
 
 
Inconclusive(2)
 
 
Unspecified(20)
 
 
Top Targets:
p450(4)
 
 
 
Menin(3)
 
 
 
DUF3652(2)
 
 
ZnF C3H1(2)
 
 
GST C Sigma(2)
 
 
 
BioAssay Types:
Literature(111)
 
 
 
 
 
Confirmatory(32)
 
 
 
 
Screening(2)
 
 
BioActivity Types:
Potency(31)
 
 
 
 
IC50(23)
 
 
 
 
Ki(11)
 
 
 
Kd(1)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 84    Data Row: 145   Total Pages: 3   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103444835]
Ki 0.00058Binding affinity to thromboxane receptor [AID551275, Type: Literature]
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2
[SID103444835]
Ki 0.0043Inhibition of [3H]PGD-2 binding to human chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) [AID239567, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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3
[SID103444835]
Ki 0.0045Inhibition of [3H]SQ-29,548 binding to human Thromboxane A2 receptor [AID238927, Type: Literature]Thromboxane A2 receptor [gi:229463010]
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4
[SID103444835]
IC50 0.0084Inhibition of beta-arrestin translocation at human Thromboxane A2 receptor in BRET assay [AID248580, Type: Literature]Thromboxane A2 receptor [gi:229463010]
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5
[SID103444835]
IC50 0.0096Inhibition of U-46,619-induced inositol phosphate accumulation at human Thromboxane A2 receptor [AID248754, Type: Literature]Thromboxane A2 receptor [gi:229463010]
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6
[SID144206069]
Potency 0.0103qHTS Assay for Inhibitors of MBNL1-poly(CUG) RNA binding: Counterscreen HTRF assay [AID651843, Type: confirmatory]MEN1 gene product [Homo sapiens] [gi:18860839]
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7
[SID50112772]
Potency 0.0116qHTS Assay for Inhibitors of MBNL1-poly(CUG) RNA binding: Initial hit validation in AlphaScreen assay for MBNL1-(CUG)12 binding [AID493205, Type: confirmatory]muscleblind-like protein 1 isoform a [Homo sapiens] [gi:41281591]
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8
[SID103444835]
Kd 0.01259Compound was tested for inhibition of U-46,619 induced contraction of isolated rabbit saphenous vein [AID166818, Type: Literature]
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9
[SID103444835]
IC50 0.014Displacement of [3H]SQ-29548 from thromboxane receptor in human platelet membrane [AID429618, Type: Literature]Thromboxane A2 receptor [gi:229463010]
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10
[SID50112772]
Potency 0.0163qHTS Assay for Inhibitors of MBNL1-poly(CUG) RNA binding: Initial hit validation from the primary screen [AID493199, Type: confirmatory]muscleblind-like protein 1 isoform a [Homo sapiens] [gi:41281591]
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11
[SID103444835]
Ki 0.018Inhibitory activity for binding of PGD-2 in hTP binding assay using HEK293 cell membranes [AID244585, Type: Literature]
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12
[SID103444835]
IC50 0.021Antagonist activity against CRTh2 receptor in human eosinophils assessed as cell shape change [AID431338, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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13
[SID103444835]
IC50 0.028Inhibition of beta-arrestin translocation at human chemoattractant receptor-homologous molecule expressed on TH2 cells in BRET assay [AID248959, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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14
[SID103444835]
IC50 0.029Inhibition of PGD2-induced inositol phosphate formation at human chemoattractant receptor-homologous molecule expressed on TH2 cells [AID248926, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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15
[SID103444835]
IC50 0.05Anti-platelet activity was measured by studying their antagonist effects on human platelets aggregated with collagen [AID92808, Type: Literature]
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16
[SID103444835]
Ki 0.073Displacement of [3H]PGD2 from human CRTh2 receptor expressed in CHO cells [AID431337, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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17
[SID103444835]
IC50 0.077Displacement of [3H]PGD2 from human CRTh2 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay [AID586985, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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18
[SID103444835]
Ki 0.137Binding affinity to human recombinant CRTH2 receptor by cell based radioligand equilibrium competition assay [AID551273, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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19
[SID103444835]
IC50 0.169Antagonist activity at human CRTH2 receptor assessed as inhibition of DK-PGD2-induced eosinophil chemotaxis [AID330825, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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20
[SID103444835]
IC50 0.195Antagonist activity against CRTh2 receptor in human whole blood assessed as eosinophil shape change [AID431356, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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21
[SID103444835]
IC50 0.21Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as effect on cAMP accumulation [AID431354, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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22
[SID103444835]
Ki 0.29Inhibitory activity for binding of PGD-2 to CRTH-2 in hCRTH-2 binding assay using HEK293 cell membranes [AID244593, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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23
[SID103444835]
Ki 0.29Inhibitory activity for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium [AID244599, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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24
[SID103444835]
IC50 0.311Displacement of [3H]PGD2 from human prostaglandin D2 receptor [AID429614, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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25
[SID103444835]
Ki 0.34Inhibitory concentration for PGD2-mediated receptor activation in a fluorescence assay that measures changes in intracellular calcium [AID244604, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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26
[SID103444835]
IC50 0.38Compound was tested for inhibition of U-46,619 induced aggregation of human platelets [AID92098, Type: Literature]
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27
[SID103444835]
IC50 0.461Antagonist activity against human CRTh2 receptor expressed in CHO cells assessed as inhibition of PGD2-mediated Ca2+ flux [AID586990, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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28
[SID103444835]
IC50 0.754Displacement of [3H]PGD2 from human prostaglandin D2 receptor in presence of human serum albumin [AID429615, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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29
[SID103444835]
IC50 1.21Inhibition of eosinophil degranulation in human whole blood assessed as change in morphology after 4 mins using flow cytometry by leukocyte shape change assay [AID429616, Type: Literature]
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30
[SID103444835]
Ki 11.02Binding affinity to prostanoid DP1 receptor [AID551274, Type: Literature]
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31
[SID103444835]
IC50 15Inhibition of human CYP2C9 [AID429621, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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32
[SID103444835]
IC50 15Inhibition of human CYP2C9 [AID429621, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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33
[SID103444835]
IC50 15Inhibition of human CYP2C9 [AID429621, Type: Literature]Cytochrome P450 2C9 [gi:6686268]
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34
[SID103444835]
IC50 33.4Displacement of [3H]PGD2 from prostaglandin D1 receptor in human platelet membrane [AID429617, Type: Literature]Prostaglandin D2 receptor [gi:2495009]
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35
[SID50112772]
Potency S16 Schwann cell PMP22 intronic element beta-lactamase assay [AID624044, Type: confirmatory]Pmp22 gene product [Rattus norvegicus] [gi:8393992]
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36
[SID103444835]
IC50 10Inhibition of PGD2-induced inositol phosphate formation at human Prostaglandin D2 receptor [AID248439, Type: Literature]Prostaglandin D2 receptor [gi:2495009]
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37
[SID103444835]
Ki 10Inhibition of [3H]-PGD-2 binding to human Prostaglandin D2 receptor [AID238910, Type: Literature]Prostaglandin D2 receptor [gi:2495009]
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38
[SID103444835]
IC50 30Inhibition of human CYP2D6 [AID429622, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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39
[SID103444835]
IC50 30Inhibition of human CYP2D6 [AID429622, Type: Literature]Cytochrome P450 2D6 [gi:84028191]
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40
[SID103444835]
IC50 30Inhibition of human CYP3A4 [AID429620, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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41
[SID103444835]
IC50 30Inhibition of human CYP3A4 [AID429620, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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42
[SID103444835]
IC50 30Inhibition of human CYP3A4 [AID429620, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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43
[SID103444835]
IC50 100Displacement of [3H]iloprost from human prostacyclin receptor expressed in human 293 cell membrane [AID429619, Type: Literature]Prostacyclin receptor [gi:1172500]
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44
[SID103444835]
 Compound was tested for inhibition of U-46,619 induced increase in tracheal pressure of guinea pigs [AID76697, Type: Literature]
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45
[SID103444835]
 Lipophilicity, log D of the compound at pH 7.4 [AID586986, Type: Literature]
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46
[SID103444835]
 Agonist activity at CRTh2 receptor in human whole blood assessed as eosinophil shape change by fluorescence assay relative to 13,14-dihydro-15-keto-PGD2 [AID586989, Type: Literature]Prostaglandin D2 receptor 2 [gi:296439334]
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47
[SID103444835]
 Percentage inhibition for binding of PGD-2 in hTP binding assay using HEK293 cell membranes [AID251891, Type: Literature]Thromboxane A2 receptor [gi:229463010]
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48
[SID103444835]
 Induction of CYP3A4 activity in cryopreserved human hepatocytes at 10 uM using midazolam as substrate after 2 days relative to rifampicin [AID429623, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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49
[SID103444835]
 Induction of CYP3A4 activity in cryopreserved human hepatocytes at 10 uM using midazolam as substrate after 2 days relative to rifampicin [AID429623, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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50
[SID103444835]
 Induction of CYP3A4 activity in cryopreserved human hepatocytes at 10 uM using midazolam as substrate after 2 days relative to rifampicin [AID429623, Type: Literature]Cytochrome P450 3A4 [gi:116241312]
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