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GW 4064 (CID 9893571) - Compound BioActivity Data
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BioActivity Outcomes:
Active(45)
 
 
Inactive(32)
 
 
Inconclusive(8)
 
 
Unspecified(24)
 
 
Top Targets:
NR LBD Fxr(37)
 
 
 
 
HELICc(3)
 
 
ABC MTABC3 MD..(2)
 
 
Bromo ALL-1(2)
 
 
 
Menin(2)
 
 
 
BioAssay Types:
Literature(53)
 
 
 
 
 
Confirmatory(38)
 
 
 
 
Screening(14)
 
 
 
BioActivity Types:
Potency(39)
 
 
 
 
EC50(22)
 
 
IC50(2)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 105    Data Row: 109   Total Pages: 3   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103317356]
EC50 0.015Agonist activity at FXR [AID694036, Type: Literature]
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2
[SID103317356]
EC50 0.015Ligand dependent recruitment of SRC1(676-700) peptide to human Farnesoid X-activated receptor by fluorescence resonance energy transfer assay [AID72529, Type: Literature]Bile acid receptor [gi:46577705]
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3
[SID103317356]
EC50 0.02Agonist activity at human GST-fused FXR LBD assessed as cofactor peptide interaction with receptor ligand binding domain by FRET assay [AID494859, Type: Literature]Bile acid receptor [gi:46577705]
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4
[SID103317356]
EC50 0.03Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay [AID494863, Type: Literature]Bile acid receptor [gi:46577705]
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5
[SID103317356]
EC50 0.035Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay [AID494861, Type: Literature]Bile acid receptor [gi:46577705]
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6
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
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7
[SID103317356]
EC50 0.059Agonist activity at human FXR assessed as SRC1 peptide interaction with receptor ligand binding domain by FRET assay [AID352768, Type: Literature]Bile acid receptor [gi:46577705]
View
8
[SID103317356]
EC50 0.059Induction of SRC1 coactivator peptide binding to ligand binding domain of human FXR by FRET assay [AID433264, Type: Literature]Bile acid receptor [gi:46577705]
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9
[SID103317356]
EC50 0.059Agonist activity at FXR assessed as receptor-SRC-1 peptide interaction by FRET assay [AID341960, Type: Literature]
View
10
[SID103317356]
EC50 0.059Agonist activity at human FXR LBD assessed as SRC1 peptide recruitment by FRET assay [AID577551, Type: Literature]Bile acid receptor [gi:46577705]
View
11
[SID103317356]
EC50 0.059Agonist activity at human amino-terminal polyhistidine-tagged FXR alpha LBD (amino acids 237 to 472) assessed as cofactor peptide SRC-1 interaction with receptor ligand binding domain after 2 hrs by FRET assay [AID622453, Type: Literature]Bile acid receptor [gi:46577705]
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12
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, Type: Literature]Bile acid receptor [gi:46577705]
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13
[SID103317356]
EC50 0.065Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells [AID433266, Type: Literature]Bile acid receptor [gi:46577705]
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14
[SID103317356]
EC50 0.065Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay [AID352765, Type: Literature]Bile acid receptor [gi:46577705]
View
15
[SID103317356]
EC50 0.065Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay [AID341962, Type: Literature]
View
16
[SID103317356]
EC50 0.065Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay [AID622454, Type: Literature]Bile acid receptor [gi:46577705]
View
17
[SID103317356]
EC50 0.065Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression [AID577553, Type: Literature]Bile acid receptor [gi:46577705]
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18
[SID103317356]
EC50 0.07Activation of human farnesoid X receptor [AID240068, Type: Literature]Bile acid receptor [gi:46577705]
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19
[SID103317356]
EC50 0.07Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity [AID294203, Type: Literature]Bile acid receptor [gi:46577705]
View
20
[SID103317356]
EC50 0.07Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay [AID662692, Type: Literature]Bile acid receptor [gi:46577705]
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21
[SID103317356]
IC50 0.112Displacement of radioligand from human FXR by scintillation proximity assay [AID568244, Type: Literature]Bile acid receptor [gi:46577705]
View
22
[SID103317356]
EC50 0.9Agonist activity at chimeric FXR assessed as receptor transactivation by luciferase transcriptional reporter gene assay [AID352178, Type: Literature]
View
23
[SID103317356]
EC50 0.91Agonist activity at Gal4-fused human FXR by luciferase reporter gene transactivation assay [AID568245, Type: Literature]Bile acid receptor [gi:46577705]
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24
[SID103317356]
EC50 2Agonist activity at mouse chimeric FXR assessed as receptor transactivation by luciferase transcriptional reporter gene assay [AID352180, Type: Literature]Bile acid receptor [gi:341942230]
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25
[SID50112875]
Potency 5.6234VP16 counterscreen qHTS for inhibitors of ROR gamma transcriptional activity [AID2546, Type: confirmatory]nuclear receptor ROR-gamma [Mus musculus] [gi:188536040]
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26
[SID50112875]
Potency 11.7704Cytotoxicity counterscreen for NFkB agonists and antagonists [AID624476, Type: confirmatory]
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27
[SID50112875]
Potency 12.5893qHTS Assay for Inhibitors of GCN5L2 [AID504327, Type: confirmatory]histone acetyltransferase KAT2A [Homo sapiens] [gi:153791535]
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28
[SID50112875]
Potency 21.1142qHTS Assay for Identification of Small Molecule Antagonists for NFkB Signaling Pathway. [AID624479, Type: confirmatory]
View
29
[SID50112875]
Potency 29.9349qHTS for Inhibitors of Polymerase Kappa [AID588579, Type: confirmatory]DNA polymerase kappa [Homo sapiens] [gi:7705344]
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30
[SID50112875]
Potency 31.6228qHTS Assay for Inhibitors of Bloom's syndrome helicase (BLM) [AID2528, Type: confirmatory]Bloom syndrome protein isoform 1 [Homo sapiens] [gi:4557365]
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31
[SID50112875]
Potency 31.6228qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) [AID2549, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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32
[SID50112875]
Potency 35.4813Confirmation qHTS Assay for Inhibitors of RecQ-Like Dna Helicase 1 (RECQ1) - Round 2 Cherry Picks [AID504841, Type: confirmatory]Chain A, Structure Of Human Recq-Like Helicase In Complex With A Dna Substrate [gi:282403581]
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33
[SID103317356]
Binding affinity to human FXR by X-ray crystallography [AID577591, Type: Literature]Bile acid receptor [gi:46577705]
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34
[SID85788199]
Luminescence Cell-Based Primary HTS to Identify Re-Activators of the P53 Mutant Pathway Measured in Cell-Based System Using Plate Reader - 2071-01_Activator_SinglePoint_HTS_Activity [AID624151, Type: screening]
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35
[SID103317356]
Activation of BSEP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR [AID303499, Type: Literature]
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36
[SID103317356]
Activation of BSEP gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR [AID303501, Type: Literature]
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37
[SID103317356]
Activation of SHP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR [AID303503, Type: Literature]
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38
[SID103317356]
Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR [AID303509, Type: Literature]
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39
[SID103317356]
Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR [AID303510, Type: Literature]
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40
[SID50112875]
A qHTS for Small Molecule Inhibitors of Shiga Toxin [AID2315, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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41
[SID50112875]
Cycloheximide Counterscreen for Small Molecule Inhibitors of Shiga Toxin [AID2314, Type: screening]shiga toxin 1 variant A subunit [Escherichia coli O157:H7] [gi:32400299]
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42
[SID50112875]
Cycloheximide Counterscreen for Small Molecule Inhibitors of Shiga Toxin [AID2314, Type: screening]shiga toxin 1 B subunit [Escherichia coli O157:H7] [gi:32400300]
View
43
[SID50112875]
A qHTS for Small Molecule Inhibitors of Shiga Toxin [AID2315, Type: screening]shiga toxin 1 B subunit [Escherichia coli O157:H7] [gi:32400300]
View
44
[SID85788199]
EZH2/PRC2 methyltransferase inhibitors Measured in Biochemical System Using Plate Reader - 2125-01_Inhibitor_SinglePoint_HTS_Activity [AID651548, Type: screening]histone-lysine N-methyltransferase EZH2 isoform a [Homo sapiens] [gi:21361095]
View
45
[SID103317356]
Activity at human VP16-FXR assessed as activation of SRC1 interaction domain 2 recruitment at 1 uM by mammalian two-hybrid assay [AID303495, Type: Literature]Bile acid receptor [gi:46577705]
View
46
[SID103317356]
Agonist activity at human FXR assessed as SRC1 peptide interaction with receptor ligand binding domain by FRET assay relative to GW-4064 [AID352764, Type: Literature]Bile acid receptor [gi:46577705]
View
47
[SID103317356]
Farnesoid X-activated receptor activity compared to 50 uM chenodeoxycholic acid (CDCA) [AID72530, Type: Literature]Bile acid receptor [gi:46577705]
View
48
[SID103317356]
Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay relative to GW-4064 [AID352769, Type: Literature]Bile acid receptor [gi:46577705]
View
49
[SID103317356]
Agonist activity at human GST-fused FXR LBD assessed as cofactor peptide interaction with receptor ligand binding domain by FRET assay relative to GW-4064 [AID494860, Type: Literature]Bile acid receptor [gi:46577705]
View
50
[SID103317356]
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay relative to GW-4064 [AID494862, Type: Literature]Bile acid receptor [gi:46577705]
View