Compile Data Set for Download or QSAR
Report error Found 4443 of ic50 for UniProtKB: Q8NER1
LigandChemical structure of BindingDB Monomer ID 642078BDBM642078(US11845730, Example 9-peak-1)
Affinity DataIC50: 0.0900nMAssay Description:Assay buffer preparation: 1 HBSS, 2 mM HEPES, 0.1% BSA plus 2.5 mM freshly prepared probenecid (Invitrogen, #P36400). 25 μl/well assay buffer in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2024
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 20315BDBM20315(3-[(4-tert-butylphenyl)methyl]-1-[(4-methanesulfon...)
Affinity DataIC50: 0.110nMAssay Description:Antagonist activity at TRPV1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 642142BDBM642142(US11845730, Example 69)
Affinity DataIC50: 0.150nMAssay Description:Assay buffer preparation: 1 HBSS, 2 mM HEPES, 0.1% BSA plus 2.5 mM freshly prepared probenecid (Invitrogen, #P36400). 25 μl/well assay buffer in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2024
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50133817BDBM50133817(BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-...)
Affinity DataIC50: 0.150nMAssay Description:Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-b...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/25/2014
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50418189BDBM50418189(CHEMBL1761696)
Affinity DataIC50: 0.158nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO-K1 cells assessed as inhibition of capsaicin-induced intracellular Ca2+ influx by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50133817BDBM50133817(BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-...)
Affinity DataIC50: 0.180nMAssay Description:Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accum...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2016
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50323836BDBM50323836(3-(3-(trifluoromethyl)pyridin-2-yl)-N-(5-(trifluor...)
Affinity DataIC50: 0.200nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50315610BDBM50315610((4-Trifluoromethylphenyl)-[7-(3-trifluoromethylpyr...)
Affinity DataIC50: 0.210nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsazepine-induced calcium mobilization by FLIPR ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50315616BDBM50315616(3-[3-(Trifluoromethyl)pyridin-2-yl]-N-[5-(trifluor...)
Affinity DataIC50: 0.230nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsazepine-induced calcium mobilization by FLIPR ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50566150BDBM50566150(CHEMBL4781687)
Affinity DataIC50: 0.270nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50566150BDBM50566150(CHEMBL4781687)
Affinity DataIC50: 0.270nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin induced intracellular Ca2+ ions by fluor...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 20531BDBM20531(N-{6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}qui...)
Affinity DataIC50: 0.300nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50272889BDBM50272889(2-(isopropoxymethyl)-N-(4-(trifluoromethyl)phenyl)...)
Affinity DataIC50: 0.300nMAssay Description:Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50170047BDBM50170047((4-Hydroxy-3-iodo-5-methoxy-phenyl)-acetic acid (2...)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 210898BDBM210898(US9273043, A126(e))
Affinity DataIC50: 0.400nMpH: 7.2 T: 2°CAssay Description:pH dependent Ca2+ responses in TRPV1/CHO cells cultured in a 96-well plate were determined (see, e.g., FIG. 2 of U.S. Patent Application Publication ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/30/2017
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 210894BDBM210894(US9273043, A123(e))
Affinity DataIC50: 0.400nMpH: 7.2 T: 2°CAssay Description:pH dependent Ca2+ responses in TRPV1/CHO cells cultured in a 96-well plate were determined (see, e.g., FIG. 2 of U.S. Patent Application Publication ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/30/2017
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50272976BDBM50272976(2-((2,6-dimethylmorpholino)methyl)-N-(4-(trifluoro...)
Affinity DataIC50: 0.400nMAssay Description:Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 20464BDBM20464((2E)-3-[2-(piperidin-1-yl)-6-(trifluoromethyl)pyri...)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 642176BDBM642176(US11845730, Example 103)
Affinity DataIC50: 0.440nMAssay Description:Assay buffer preparation: 1 HBSS, 2 mM HEPES, 0.1% BSA plus 2.5 mM freshly prepared probenecid (Invitrogen, #P36400). 25 μl/well assay buffer in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2024
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50621014BDBM50621014(CHEMBL5406113)
Affinity DataIC50: 0.460nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsaicin induced intracellular Ca2+ ions by fluor...More data for this Ligand-Target Pair
Ligand InfoSimilars
In Depth
Date in BDB:
12/15/2024
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 50272890BDBM50272890(2-(benzyloxymethyl)-N-(4-(trifluoromethyl)phenyl)-...)
Affinity DataIC50: 0.5nMAssay Description:Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 185339BDBM185339(US9156830, I-7)
Affinity DataIC50: 0.5nMpH: 7.4Assay Description:Two days prior to performing this assay, cells are seeded on poly-D-lysine-coated 96-well clear-bottom black plates (commercially available from Bect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/30/2016
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50272848BDBM50272848(2-methyl-N-(4-(trifluoromethyl)phenyl)-7-(3-(trifl...)
Affinity DataIC50: 0.5nMAssay Description:Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50336144BDBM50336144((1R,3S)-4-chloro-N-(3-hydroxycyclohexyl)-5-(4-(tri...)
Affinity DataIC50: 0.501nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50061298BDBM50061298(CHEMBL3393837)
Affinity DataIC50: 0.550nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of 45 degC heat-induced effect at 1 uM by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/4/2016
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 642080BDBM642080(US11845730, Example 9-racemic)
Affinity DataIC50: 0.580nMAssay Description:Assay buffer preparation: 1 HBSS, 2 mM HEPES, 0.1% BSA plus 2.5 mM freshly prepared probenecid (Invitrogen, #P36400). 25 μl/well assay buffer in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2024
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50372585BDBM50372585(CHEMBL404165)
Affinity DataIC50: 0.580nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50133817BDBM50133817(BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-...)
Affinity DataIC50: 0.600nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 20557BDBM20557(N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl...)
Affinity DataIC50: 0.600nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of low pH-induced calcium influxMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 210896BDBM210896(US9273043, A125(e))
Affinity DataIC50: 0.600nMpH: 7.2 T: 2°CAssay Description:pH dependent Ca2+ responses in TRPV1/CHO cells cultured in a 96-well plate were determined (see, e.g., FIG. 2 of U.S. Patent Application Publication ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/30/2017
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 20531BDBM20531(N-{6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl}qui...)
Affinity DataIC50: 0.600nMpH: 7.4 T: 2°CAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50133817BDBM50133817(BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-...)
Affinity DataIC50: 0.600nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK293 cells assessed as blockade of acid-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 20557BDBM20557(N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl...)
Affinity DataIC50: 0.620nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 642074BDBM642074(US11845730, Example 7-peak-1)
Affinity DataIC50: 0.620nMAssay Description:Assay buffer preparation: 1 HBSS, 2 mM HEPES, 0.1% BSA plus 2.5 mM freshly prepared probenecid (Invitrogen, #P36400). 25 μl/well assay buffer in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2024
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50372585BDBM50372585(CHEMBL404165)
Affinity DataIC50: 0.620nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50315608BDBM50315608((4-Trifluoromethylphenyl)-[7-(3-trifluoromethylpyr...)
Affinity DataIC50: 0.630nMAssay Description:Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed as inhibition of capsazepine-induced calcium mobilization by FLIPR ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/30/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50418959BDBM50418959(CHEMBL1807875)
Affinity DataIC50: 0.631nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50418961BDBM50418961(CHEMBL1807877)
Affinity DataIC50: 0.631nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of calcium flux by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50566185BDBM50566185(CHEMBL4787931)
Affinity DataIC50: 0.640nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50372585BDBM50372585(CHEMBL404165)
Affinity DataIC50: 0.650nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50372586BDBM50372586(CHEMBL255420)
Affinity DataIC50: 0.650nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50232114BDBM50232114(N-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'...)
Affinity DataIC50: 0.700nMpH: 5.5Assay Description:Blockade of pH 5.5-induced activation of TRPV1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/11/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50133817BDBM50133817(BCTC | CHEMBL441472 | N-(4-tert-butylphenyl)-4-(3-...)
Affinity DataIC50: 0.700nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50566168BDBM50566168(CHEMBL4789232)
Affinity DataIC50: 0.75nMAssay Description:Antagonist activity at human TRPV1 expressed in HEK cells assessed as inhibition of 10 nM capsaicin-induced calcium uptake by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/30/2022
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 20557BDBM20557(N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl...)
Affinity DataIC50: 0.760nMAssay Description:TRPV1 activities were monitored as a function of cellular uptake of radioactive calcium (45Ca2+). The test compounds were preincubated with TRPV1 exp...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2008
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 20557BDBM20557(N-[4-({6-[4-(trifluoromethyl)phenyl]pyrimidin-4-yl...)
Affinity DataIC50: 0.760nMAssay Description:Antagonist activity at human TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium mobilizationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/15/2012
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50323839BDBM50323839(5-(trifluoromethyl)-6-(8-(5-(trifluoromethyl)pyrid...)
Affinity DataIC50: 0.800nMAssay Description:Antagonist activity at human TRPV1 assessed as inhibition of capsaicin-induced receptor activation by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/19/2011
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50398494BDBM50398494(CHEMBL2177429)
Affinity DataIC50: 0.800nMAssay Description:Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of 45 degC heat-induced activity after 5 mins by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/13/2014
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50398494BDBM50398494(CHEMBL2177429)
Affinity DataIC50: 0.800nMAssay Description:Antagonist activity at human TRPV1 expressed in CHOK1 cells assessed as inhibition of heat-induced activity after 5 mins by FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2013
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 236215BDBM236215(US9365563, K6 | US9878991, Compound K6)
Affinity DataIC50: 0.800nMpH: 7.4Assay Description:Two days prior to performing this assay, cells are seeded on poly-D-lysine-coated 96-well clear-bottom black plates (commercially available from Bect...More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/3/2017
Entry Details
US Patent

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