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gefitinib (CID 123631) - Compound BioActivity Data
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BioActivity Outcomes:
Active(965)
 
 
Inactive(510)
 
 
Inconclusive(99)
 
 
Unspecified(750)
 
 
Top Targets:
PKc(100)
 
 
 
 
PKc like(79)
 
 
 
 
PTKc EGFR(67)
 
 
 
 
STKc AGC(43)
 
 
 
 
PTKc Abl(32)
 
 
 
 
BioAssay Types:
Literature(1483)
 
 
 
 
 
Confirmatory(192)
 
 
 
 
Screening(34)
 
 
 
Summary(25)
 
 
 
 
BioActivity Types:
Kd(882)
 
 
 
 
IC50(713)
 
 
 
 
Potency(163)
 
 
 
 
EC50(4)
 
 
Ki(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 1935    Data Row: 2324   Total Pages: 47   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103244983]
Ki 0.0004Inhibition of EGFR [AID512580, Type: Literature]
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2
[SID103244983]
Kd 0.00052Binding constant for EGFR(L747-T751del,Sins) kinase domain [AID435906, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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3
[SID103244983]
Kd 0.00052Binding constant for EGFR(L747-T751del,Sins) kinase domain [AID625002, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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4
[SID103244983]
Kd 0.00054Binding constant for EGFR(E746-A750del) kinase domain [AID624997, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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5
[SID103244983]
Kd 0.00054Binding constant for EGFR(E746-A750del) kinase domain [AID435791, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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6
[SID103244983]
Kd 0.00057Binding constant for EGFR(L747-E749del, A750P) kinase domain [AID435652, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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7
[SID103244983]
Kd 0.00057Binding constant for EGFR(L747-S752del, P753S) kinase domain [AID435653, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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8
[SID103244983]
Kd 0.00057Binding constant for EGFR(L747-E749del, A750P) kinase domain [AID625000, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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9
[SID103244983]
Kd 0.00057Binding constant for EGFR(L747-S752del, P753S) kinase domain [AID625001, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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10
[SID103244983]
Kd 0.00094Binding constant for EGFR(L858R) kinase domain [AID625003, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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11
[SID103244983]
Kd 0.00094Binding constant for EGFR(L858R) kinase domain [AID435525, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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12
[SID103244983]
Kd 0.00098Binding constant for EGFR(S752-I759del) kinase domain [AID625006, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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13
[SID103244983]
Kd 0.00098Binding constant for EGFR(S752-I759del) kinase domain [AID435792, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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14
[SID103244983]
Kd 0.001Binding constant for EGFR kinase domain [AID435156, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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15
[SID103244983]
Kd 0.001Binding constant for EGFR kinase domain [AID624996, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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16
[SID103244983]
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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17
[SID103244983]
IC50 0.001Inhibition of recombinant EGFR by radioactive phosphotransfer assay in presence of 10 uM ATP [AID507084, Type: Literature]
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18
[SID103244983]
IC50 0.001Inhibition of EGFR by homogeneous time-resolved fluorescence assay [AID580190, Type: Literature]
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19
[SID103244983]
IC50 0.001Inhibitory activity against epidermal growth factor receptor [AID69892, Type: Literature]
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20
[SID103244983]
IC50 0.001Inhibition of EGFR [AID463638, Type: Literature]
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21
[SID103244983]
Kd 0.0011Binding constant for EGFR(G719S) kinase domain [AID624999, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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22
[SID103244983]
Kd 0.0011Binding constant for EGFR(G719S) kinase domain [AID435402, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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23
[SID103244983]
Kd 0.0014Binding constant for EGFR(L861Q) kinase domain [AID435907, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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24
[SID103244983]
Kd 0.0014Binding constant for EGFR(L861Q) kinase domain [AID625005, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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25
[SID103244983]
IC50 0.0015Cytotoxicity against human HCC827 cells incubated for 72 hrs by MTT assay [AID708982, Type: Literature]
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26
[SID103244983]
Kd 0.0018Average Binding Constant for EGFR ; NA=Not Active at 10 uM [AID256664, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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27
[SID103244983]
Kd 0.002Binding constant for EGFR(G719C) kinase domain [AID435157, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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28
[SID103244983]
Kd 0.002Binding constant for EGFR(G719C) kinase domain [AID624998, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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29
[SID103244983]
Kd 0.0024Binding affinity to EGFR with L858R mutant [AID394660, Type: Literature]
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30
[SID103244983]
IC50 0.0031Inhibition of erbB1 fusion protein expressed in baculovirus by ELISA [AID260895, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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31
[SID29215403]
Potency 0.0032Assay 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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32
[SID29215403]
Potency 0.0032Assay 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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33
[SID29215403]
EGFR IC50 0.004Quantitative 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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34
[SID103244983]
IC50 0.0042Inhibition of EGFR after 1 hrs by luminescence assay [AID611842, Type: Literature]
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35
[SID103244983]
IC50 0.00517SANGER: Inhibition of human EoL-1-cell cell growth in a cell viability assay. [AID742166, Type: other]
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36
[SID103244983]
IC50 0.0054Inhibition of human EGFR in presence of 1 uM ATP [AID295762, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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37
[SID103244983]
Kd 0.007Average Binding Constant for GAK ; NA=Not Active at 10 uM [AID256612, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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38
[SID103244983]
IC50 0.0073Inhibition of EGFR after 50 mins by HTRF assay [AID644746, Type: Literature]
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39
[SID103244983]
IC50 0.008Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay [AID662596, Type: Literature]
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40
[SID103244983]
EC50 0.01Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining [AID410945, Type: Literature]
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41
[SID103244983]
IC50 0.0108Cytotoxicity against mouse BA/F3 cells expressing EGFR L858R mutant [AID394662, Type: Literature]
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42
[SID103244983]
Kd 0.0109Binding affinity to EGFR with L858R/T790M mutant [AID394661, Type: Literature]
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43
[SID103244983]
IC50 0.012Antiproliferative activity against human HCC827 cells after 96 hrs by MTS assay [AID492111, Type: Literature]
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44
[SID103244983]
IC50 0.013Antiproliferative activity against human HCC827 cells by MTS assay [AID528339, Type: Literature]
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45
[SID103244983]
Kd 0.013Binding constant for GAK kinase domain [AID435821, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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46
[SID103244983]
Kd 0.013Binding constant for GAK kinase domain [AID625012, Type: Literature]Cyclin-G-associated kinase [gi:17375734]
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47
[SID103244983]
IC50 0.014Cytotoxicity against human PC9 cells incubated for 72 hrs by MTT assay [AID708803, Type: Literature]
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48
[SID103244983]
IC50 0.0144Inhibition of EGF stimulated human erbB1 autophosphorylation in NIH3T3 cells [AID260898, Type: Literature]Epidermal growth factor receptor [gi:2811086]
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49
[SID103244983]
IC50 0.015Inhibition of human GST-tagged EGFR L834R mutant expressed in Sf9 cells by luminescence assay [AID739694, Type: Literature]
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50
[SID103244983]
EC50 0.017Antiproliferative activity against EGFR-deficient human PC9 cells [AID552132, Type: Literature]
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