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erlotinib (CID 176870) - Compound BioActivity Data
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BioActivity Outcomes:
Active(565)
 
 
Inactive(423)
 
 
Inconclusive(79)
 
 
Unspecified(1487)
 
 
Top Targets:
PKc(96)
 
 
 
 
PKc like(80)
 
 
 
 
 
PTKc EGFR(60)
 
 
 
 
 
STKc AGC(46)
 
 
 
 
PTKc Abl(39)
 
 
 
BioAssay Types:
Literature(1980)
 
 
 
 
 
Confirmatory(202)
 
 
 
 
Summary(25)
 
 
 
 
Screening(8)
 
 
 
BioActivity Types:
Kd(885)
 
 
 
 
IC50(526)
 
 
 
 
 
Potency(144)
 
 
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 2250    Data Row: 2554   Total Pages: 52   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103177459]
IC50 0.0001Inhibition of EGFR Leu858Arg mutant by HTRF assay [AID473322, Type: Literature]
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2
[SID103177459]
IC50 0.0002Inhibition of wild type EGFR by HTRF assay [AID473321, Type: Literature]
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3
[SID103177459]
Kd 0.00035Binding constant for EGFR(L747-T751del,Sins) kinase domain [AID435906, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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4
[SID103177459]
Kd 0.00035Binding constant for EGFR(L747-T751del,Sins) kinase domain [AID625002, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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5
[SID103177459]
IC50 0.0004Inhibition of EGFR [AID383062, Type: Literature]
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6
[SID103177459]
Kd 0.00047Binding constant for EGFR(L747-S752del, P753S) kinase domain [AID435653, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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7
[SID103177459]
Kd 0.00047Binding constant for EGFR(L747-S752del, P753S) kinase domain [AID625001, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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8
[SID103177459]
Kd 0.00048Binding constant for EGFR(E746-A750del) kinase domain [AID624997, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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9
[SID103177459]
Kd 0.00048Binding constant for EGFR(E746-A750del) kinase domain [AID435791, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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10
[SID103177459]
Kd 0.00052Binding constant for EGFR(G719S) kinase domain [AID624999, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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11
[SID103177459]
Kd 0.00052Binding constant for EGFR(L747-E749del, A750P) kinase domain [AID625000, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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12
[SID103177459]
Kd 0.00052Binding constant for EGFR(G719S) kinase domain [AID435402, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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13
[SID103177459]
Kd 0.00052Binding constant for EGFR(L747-E749del, A750P) kinase domain [AID435652, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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14
[SID103177459]
IC50 0.0006Inhibition of erbB1 fusion protein expressed in baculovirus by ELISA [AID260895, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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15
[SID103177459]
Kd 0.00067Binding constant for EGFR kinase domain [AID435156, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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16
[SID103177459]
Kd 0.00067Binding constant for EGFR kinase domain [AID624996, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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17
[SID26757996]
Potency 0.0008Assay for Inhibitors of the ERK Signaling Pathway using a Homogeneous Screening Assay: EGFR Kinase Inhibition [AID1731, Type: confirmatory]epidermal growth factor receptor isoform a precursor [Homo sapiens] [gi:29725609]
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18
[SID103177459]
Kd 0.00085Binding constant for EGFR(G719C) kinase domain [AID624998, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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19
[SID103177459]
Kd 0.00085Binding constant for EGFR(G719C) kinase domain [AID435157, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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20
[SID26757996]
Potency 0.0009Assay for Inhibitors of the ERK Signaling Pathway using a Homogeneous Screening Assay: EGFR L858R Kinase Inhibition [AID1727, Type: confirmatory]epidermal growth factor receptor isoform a precursor [Homo sapiens] [gi:29725609]
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21
[SID103177459]
Kd 0.00097Binding constant for EGFR(L858R) kinase domain [AID625003, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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22
[SID103177459]
Kd 0.00097Binding constant for EGFR(L858R) kinase domain [AID435525, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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23
[SID103177459]
IC50 0.001Inhibition of EGFR phosphorylation in EGF-stimulated human A431 after 2 hrs by Western blot analysis [AID638084, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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24
[SID103177459]
IC50 0.001Inhibition of EGFR by homogeneous time-resolved fluorescence assay [AID580190, Type: Literature]
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25
[SID26757996]
EGFR IC50 0.001Quantitative High-Throughput Screen for Inhibitors of the ERK Signaling Pathway using a Homogeneous Screening Assay: Summary [AID1742, Type: summary]epidermal growth factor receptor isoform a precursor [Homo sapiens] [gi:29725609]
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26
[SID103177459]
IC50 0.001Inhibitory activity against epidermal growth factor receptor [AID69892, Type: Literature]
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27
[SID103177459]
IC50 0.001Inhibition of human EGFR [AID371183, Type: Literature]
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28
[SID103177459]
Kd 0.0012Binding constant for EGFR(L861Q) kinase domain [AID625005, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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29
[SID103177459]
Kd 0.0012Binding constant for EGFR(L861Q) kinase domain [AID435907, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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30
[SID103177459]
Kd 0.0014Average Binding Constant for EGFR ; NA=Not Active at 10 uM [AID256664, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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31
[SID103177459]
Kd 0.0016Binding constant for EGFR(S752-I759del) kinase domain [AID435792, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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32
[SID103177459]
Kd 0.0016Binding constant for EGFR(S752-I759del) kinase domain [AID625006, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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33
[SID103177459]
IC50 0.002Inhibition of EGFR [AID463638, Type: Literature]
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34
[SID103177459]
Kd 0.0031Binding constant for GAK kinase domain [AID435821, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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35
[SID103177459]
Kd 0.0031Binding constant for GAK kinase domain [AID625012, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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36
[SID103177459]
IC50 0.0031Inhibition of EGFR using poly(Glu,Tyr)4:1 as substrate and [gamma33P]ATP after 60 mins by scintillation counting [AID634136, Type: Literature]
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37
[SID103177459]
IC50 0.0036Inhibition of EGFR [AID381969, Type: Literature]
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38
[SID103177459]
IC50 0.01Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay [AID456101, Type: Literature]
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39
[SID103177459]
IC50 0.0125Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant [AID394662, Type: Literature]
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40
[SID103177459]
Kd 0.019Binding constant for LOK kinase domain [AID625030, Type: Literature]Serine/threonine-protein kinase 10 [gi:12643358]
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41
[SID103177459]
Kd 0.019Binding constant for LOK kinase domain [AID435677, Type: Literature]Serine/threonine-protein kinase 10 [gi:12643358]
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42
[SID103177459]
IC50 0.0193Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells [AID260898, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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43
[SID103177459]
IC50 0.02Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay [AID456092, Type: Literature]
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44
[SID103177459]
IC50 0.02Inhibition of cloned EGFR autophosphorylation expressed in baculovirus-infected Sf9 cells by solid-phase ELISA [AID456099, Type: Literature]
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45
[SID103177459]
IC50 0.02Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay [AID460691, Type: Literature]
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46
[SID103177459]
IC50 0.02Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay [AID616547, Type: Literature]
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47
[SID103177459]
IC50 0.02Inhibition of recombinant EGFR expressed in Sf9-baculovirus system by ELISA [AID460689, Type: Literature]
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48
[SID103177459]
IC50 0.02Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay [AID492037, Type: Literature]
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49
[SID103177459]
IC50 0.02Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay [AID492322, Type: Literature]
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50
[SID103177459]
IC50 0.02Inhibition of EGFR by HTRF assay [AID410943, Type: Literature]
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