GW 4064 (CID 9893571) - BioAssay Data Summary for Compound
.
BioActivity Outcomes:
Active(42)
 
 
Inactive(27)
 
 
Inconclusive(5)
 
 
Unspecified(24)
 
 
Top Targets:
NR LBD Fxr(35)
 
 
 
 
HELICc(3)
 
 
RIP(2)
 
 
Menin(2)
 
 
 
NR LBD ROR li..(2)
 
 
 
BioAssay Types:
Literature(51)
 
 
 
 
Confirmatory(31)
 
 
 
 
Screening(12)
 
 
 
BioActivity Types:
Potency(31)
 
 
 
 
EC50(21)
 
 
IC50(2)
 
 
SAR
Target summary
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 98    Data Row: 98   Total Pages: 2   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[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
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 0.015Ligand 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
4
[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
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]
View
6
[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]
View
7
[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]
View
8
[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]
View
9
[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
10
[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
11
[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
12
[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
13
[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
14
[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
15
[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
16
[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
17
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
View
18
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
View
19
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
View
20
[SID103317356]
EC50 0.037Effective concentration against Farnesoid X receptor (FXR) [AID72526, Type: Literature]Bile acid receptor [gi:46577705]
View
21
[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
22
[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
23
[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
24
[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
25
[SID103317356]
EC50 0.059Agonist activity at FXR assessed as receptor-SRC-1 peptide interaction by FRET assay [AID341960, Type: Literature]
View
26
[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
27
[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
28
[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
29
[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
30
[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
31
[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
32
[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
33
[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
34
[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
35
[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
36
[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
37
[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
38
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, Type: Literature]Bile acid receptor [gi:46577705]
View
39
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, Type: Literature]Bile acid receptor [gi:46577705]
View
40
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, Type: Literature]Bile acid receptor [gi:46577705]
View
41
[SID103317356]
IC50 0.064Displacement of radioligand from human FXR by scintillation proximity assay [AID352177, Type: Literature]Bile acid receptor [gi:46577705]
View
42
[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]
View
43
[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]
View
44
[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]
View
45
[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]
View
46
[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
47
[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
48
[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
49
[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
50
[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]
View