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BioActivity Data for Compound GW 4064 (CID 9893571)

BioActivity Outcomes:
Active(61)
 
 
Inactive(36)
 
 
Inconclusive(9)
 
 
Unspecified(27)
 
 
Top Targets:
NR LBD Fxr(48)
 
 
 
 
HELICc(3)
 
 
ePHD KMT2A(2)
 
 
 
SLT beta(2)
 
 
RIP(2)
 
 
BioAssay Types:
Literature(71)
 
 
 
 
 
Confirmatory(47)
 
 
 
 
Screening(14)
 
 
 
BioAssay Categories:
In vitro(5)
 
 
 
In vivo(1)
 
 
Biochemical(40)
 
 
 
 
Toxicity(2)
 
 
 
ADME(3)
 
 
Cell-based(25)
 
 
 
 
BioActivity Types:
Potency(49)
 
 
 
 
EC50(29)
 
 
IC50(5)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 128    Data Row: 133   Total Pages: 7   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103317356]
EC50 0.015Agonist activity at FXR [AID694036, Type: Literature]
View
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]
View
3
[SID103317356]
EC50 0.015Agonist activity at FXR (unknown origin) by coactivator recruitment assay [AID1138961, Type: Literature]Bile acid receptor [gi:46577705]
View
4
[SID103317356]
IC50 0.0198Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assay [AID1142317, Type: Literature]Bile acid receptor [gi:46577705]
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5
[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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6
[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]
View
7
[SID103317356]
EC50 0.03Binding affinity for human Farnesoid X receptor in FRET assay [AID240176, Type: Literature]Bile acid receptor [gi:46577705]
View
8
[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]
View
9
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
View
10
[SID103317356]
EC50 0.045Agonist activity at human FXR assessed as recruitment of SRC1 peptide by TR-FRET assay [AID755462, Type: Literature]Bile acid receptor [gi:46577705]
View
11
[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]
View
12
[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
13
[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]
View
14
[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
15
[SID103317356]
EC50 0.059Agonist activity at FXR assessed as receptor-SRC-1 peptide interaction by FRET assay [AID341960, Type: Literature]
View
16
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, 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 0.065Agonist 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
19
[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
20
[SID103317356]
EC50 0.065Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay [AID341962, Type: Literature]
View