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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
(change energy unit to
kcal/mol
)
Found
56
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Target
Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.10E+3nM
Assay Description:
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
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Target
Solute carrier organic anion transporter family member 1B3
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.40E+3nM
Assay Description:
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillatio...
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Target
Solute carrier organic anion transporter family member 1A4
(Rattus norvegicus)
University Of Zurich
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.40E+3nM
Assay Description:
TP_TRANSPORTER: inhibition of E217betaG uptake in Xenopus laevis oocytes
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Target
Solute carrier organic anion transporter family member 1A4
(Rattus norvegicus)
University Of Zurich
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.46E+3nM
Assay Description:
TP_TRANSPORTER: inhibition of Digoxin uptake in Oatp2-expressing LLC-PK1 cells
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Target
Solute carrier organic anion transporter family member 1B3
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 5.00E+3nM
Assay Description:
TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes
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Target
Bile salt export pump
(Rattus norvegicus)
University Hospital
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.19E+4nM
Assay Description:
TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells
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Target
Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.70E+4nM
Assay Description:
TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes
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Solute carrier organic anion transporter family member 1A1
(Rattus norvegicus)
Kitasato University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 1.82E+4nM
Assay Description:
TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing LLC-PK1 cells
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Solute carrier organic anion transporter family member 1A2
(Homo sapiens (Human))
University Hospital
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 5.10E+4nM
Assay Description:
TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes
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Solute carrier organic anion transporter family member 2B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 6.30E+4nM
Assay Description:
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation coun...
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Target
Arylacetamide deacetylase
(Homo sapiens (Human))
Kanazawa University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 2.00E+5nM
Assay Description:
Inhibition of AADAC in human liver microsome
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Arylacetamide deacetylase
(Homo sapiens (Human))
Kanazawa University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 3.00E+5nM
Assay Description:
Inhibition of human recombinant AADAC
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Arylacetamide deacetylase
(Homo sapiens (Human))
Kanazawa University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Ki: 7.00E+5nM
Assay Description:
Inhibition of AADAC in human jejunum microsome
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Target
Enoyl-[acyl-carrier-protein] reductase [NADH]
(Mycobacterium tuberculosis (strain ATCC 25618 / H3...)
Astrazeneca
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 30nM
Assay Description:
Inhibition of Mycobacterium tuberculosis InhA using NADH and dodecyl coA substrate by LC-MS/MS method
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Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 300nM
Assay Description:
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
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Target
NH(3)-dependent NAD(+) synthetase
(Bacillus subtilis)
University Of Alabama At Birmingham
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: >1.00E+3nM
Assay Description:
Inhibitory activity against Bacillus subtilis NAD synthetase
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Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 1.20E+3nM
Assay Description:
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting
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Solute carrier organic anion transporter family member 1B3
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 1.50E+3nM
Assay Description:
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillatio...
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Target
Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 2.20E+3nM
Assay Description:
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
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Solute carrier organic anion transporter family member 1B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 2.30E+3nM
Assay Description:
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
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Target
Alpha-synuclein
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 7.10E+3nM
Assay Description:
Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay
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Target
Cholesterol side-chain cleavage enzyme, mitochondrial
(Rattus norvegicus)
The University Of Queensland
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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IC50: <1.00E+4nM
Assay Description:
Antibacterial activity against Enterococcus faecalis incubated for 16 to 24 hrs in presence of ampicillin by broth microdilution based spectrophotome...
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Bile salt export pump
(Homo sapiens (Human))
Astrazeneca
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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IC50: 1.13E+4nM
Assay Description:
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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Bile salt export pump
(Homo sapiens (Human))
Astrazeneca
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 1.87E+4nM
Assay Description:
Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-...
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Bile salt export pump
(Homo sapiens (Human))
Astrazeneca
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 2.53E+4nM
Assay Description:
Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...
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Bile salt export pump
(Homo sapiens (Human))
Astrazeneca
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 2.53E+4nM
Assay Description:
Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...
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Lanosterol 14-alpha demethylase
(Homo sapiens (Human))
Act
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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IC50: 3.00E+4nM
Assay Description:
Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay
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Bile salt export pump
(Rattus norvegicus)
University Hospital
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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IC50: 3.47E+4nM
Assay Description:
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...
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ATP-binding cassette sub-family C member 4
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 4.19E+4nM
Assay Description:
Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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Alpha-synuclein
(Homo sapiens (Human))
Universit£
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 4.62E+4nM
Assay Description:
Inhibition of human alpha-synuclein filament formation expressed in Escherichia coli BL21(DE3) cells incubated for 72 hrs by thioflavin S based fluor...
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DNA gyrase subunit B
(Mycobacterium tuberculosis (strain ATCC 25618 / H3...)
Institute Of Technology & Science-Pilani
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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IC50: >5.00E+4nM
Assay Description:
Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis
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ATP-binding cassette sub-family C member 2
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 5.30E+4nM
Assay Description:
Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...
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Target
Broad substrate specificity ATP-binding cassette transporter ABCG2
(Homo sapiens (Human))
Federal University Of Parana
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 5.60E+4nM
Assay Description:
Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S fo...
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Solute carrier organic anion transporter family member 2B1
(Homo sapiens (Human))
Uppsala University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 6.50E+4nM
Assay Description:
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation coun...
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ATP-binding cassette sub-family C member 3
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 6.90E+4nM
Assay Description:
Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...
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Glutathione S-transferase omega-1
(Homo sapiens (Human))
Monash University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 7.50E+4nM
Assay Description:
Inhibition of GSTO1-1 (unknown origin) by enzymatic assay
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Target
Co-chaperonin GroES
(Escherichia coli)
Indiana University School Of Medicine
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed ...
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Co-chaperonin GroES
(Escherichia coli)
Indiana University School Of Medicine
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed ...
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Target
60 kDa heat shock protein, mitochondrial
(Homo sapiens)
Indiana University School Of Medicine
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Roset...
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Thiosulfate sulfurtransferase
(Homo sapiens)
Indiana University School Of Medicine
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: >1.00E+5nM
Assay Description:
Inhibition of refolded rhodanese (unknown origin) preincubated with Escherichia coli GroEL/GroES for 60 mins in absence of compound followed by compo...
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Target
DNA-directed RNA polymerase subunit beta
(Escherichia coli)
The Pennsylvania State University
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 1.71E+5nM
Assay Description:
Inhibition of rifamycin-resistant Escherichia coli RNA polymerase S531L mutant after 10 mins by rolling circle transcription assay in presence of DNA...
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DNA-directed RNA polymerase subunit beta
(Escherichia coli)
The Pennsylvania State University
Curated by
ChEMBL
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BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 2.33E+5nM
Assay Description:
Inhibition of rifamycin-resistant Escherichia coli RNA polymerase D516V mutant after 10 mins by rolling circle transcription assay in presence of DNA...
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DNA-directed RNA polymerase subunit beta
(Escherichia coli)
The Pennsylvania State University
Curated by
ChEMBL
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BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
IC50: 1.13E+6nM
Assay Description:
Inhibition of rifamycin-resistant Escherichia coli RNA polymerase H526Y mutant after 10 mins by rolling circle transcription assay in presence of DNA...
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 1.17E+3nM
Assay Description:
Agonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as transcriptional activat...
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 1.40E+3nM
Assay Description:
Agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs by lucifer...
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Target
Cytochrome P450 2B6
(Homo sapiens (Human))
Amgen
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 1.30E+3nM
Assay Description:
Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method
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Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 2.00E+3nM
Assay Description:
Agonist activity at VP16-fused human PXR expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 1.19E+3nM
Assay Description:
Activation of human PXR
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 2.30E+3nM
Assay Description:
Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 5.60E+3nM
Assay Description:
Activation of human PXR in DPX2 cells after 24 hrs by microplate reader relative to control
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 190nM
Assay Description:
Agonist activity at PXR expressed in human HepG2 cells after 24 hrs by p3A4-luciferase reporter gene assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 1.10E+3nM
Assay Description:
Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 200nM
Assay Description:
Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 3.50E+3nM
Assay Description:
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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Target
Nuclear receptor subfamily 1 group I member 2
(Homo sapiens (Human))
TBA
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
EC50: 3.20E+3nM
Assay Description:
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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Target
Albumin
(Homo sapiens (Human))
Cnrs-Cpbs/Umr 5236
Curated by
ChEMBL
Ligand
BDBM50370232
(BA-41166E | L-5103 | RIFAMPIN | Rifadin | Rifampic...)
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Affinity Data
Kd: 1.20E+4nM
Assay Description:
Binding affinity to first site on human serum albumin by SPR
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