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Found 721 with Last Name = 'jacobs' and Initial = 'jw'
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16292(3-N-[(2S,3S,5R)-3-amino-5-[(4-fluorophenyl)carbamo...)
Affinity DataKi:  26nM ΔG°:  -42.9kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16291(3-N-[(2S,3S,5R)-3-amino-5-{[(1S)-1-(benzylcarbamoy...)
Affinity DataKi:  33nM ΔG°:  -42.3kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16286(3-N-[(1R,3S,4S)-1-{[(1S)-1-(benzylcarbamoyl)-2-met...)
Affinity DataKi:  71nM ΔG°:  -40.4kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16287(3-N-[(1R,3S,4S)-3-amino-1-{[(1S)-1-(benzylcarbamoy...)
Affinity DataKi:  120nM ΔG°:  -39.1kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16289(3-N-[(1R,3S,4S)-1-[(4-fluorophenyl)carbamoyl]-3-hy...)
Affinity DataKi:  1.30E+3nM ΔG°:  -33.3kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16290(3-N-[(1R,3S,4S)-3-amino-1-[(4-fluorophenyl)carbamo...)
Affinity DataKi:  3.00E+3nM ΔG°:  -31.2kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBeta-secretase 1 [22-454](Homo sapiens (Human))
Sunesis

LigandPNGBDBM16288(3-N-[(1R,3R,4S)-3-amino-1-{[(1S)-1-(benzylcarbamoy...)
Affinity DataKi:  1.13E+4nM ΔG°:  -28.0kJ/molepH: 4.5 T: 2°CAssay Description:Compounds were tested for their ability to inhibit BACE-1 hydrolysis of the internally quenched fluorescent substrate FS-2. Reactions were initiated ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381823(CVD-0019453 | US10272079, Compound 002 | US1027207...)
Affinity DataIC50:  0.501nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381804(US10272079, Compound 161)
Affinity DataIC50:  0.631nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381783(US10272079, Compound 140)
Affinity DataIC50:  1.26nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM50601173(CHEMBL5176968)
Affinity DataIC50:  1.30nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381691(US10272079, Compound 48 | US10272079, Compound 65)
Affinity DataIC50:  1.41nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381826(US10272079, Compound 003)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM50601180(CHEMBL5170002)
Affinity DataIC50:  1.60nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381795(US10272079, Compound 152)
Affinity DataIC50:  2nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381710(US10272079, Compound 67)
Affinity DataIC50:  2nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM50601178(CHEMBL5202545)
Affinity DataIC50:  2nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381762(US10272079, Compound 119)
Affinity DataIC50:  2nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381826(US10272079, Compound 003)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of rat NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381742(US10272079, Compound 99)
Affinity DataIC50:  2.51nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381793(US10272079, Compound 150)
Affinity DataIC50:  2.51nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381826(US10272079, Compound 003)
Affinity DataIC50:  2.51nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381817(US10272079, Compound 174)
Affinity DataIC50:  2.51nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381667(US10272079, Compound 24)
Affinity DataIC50:  2.63nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381758(US10272079, Compound 115)
Affinity DataIC50:  2.82nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381666(US10272079, Compound 23)
Affinity DataIC50:  2.82nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381817(US10272079, Compound 174)
Affinity DataIC50:  2.95nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381740(US10272079, Compound 97)
Affinity DataIC50:  3.16nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM426615(N,N′-(10,17-dioxo-3,6,21,24-tetraoxa-9,11,16...)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of rat NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ...More data for this Ligand-Target Pair
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381778(US10272079, Compound 135)
Affinity DataIC50:  3.55nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381823(CVD-0019453 | US10272079, Compound 002 | US1027207...)
Affinity DataIC50:  3.98nMAssay Description:The ability of compounds to inhibit Rat NHE3-mediated Na+-dependent H+ antiport after application and washout was measured using a modification of th...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381809(US10272079, Compound 166)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381791(US10272079, Compound 148)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381675(US10272079, Compound 32)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381673(US10272079, Compound 30)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381670(US10272079, Compound 27)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381741(US10272079, Compound 98)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381751(US10272079, Compound 108)
Affinity DataIC50:  3.98nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAurora kinase A(Mus musculus (mouse))
Sunesis Pharmaceuticals

LigandPNGBDBM26333(1-[3-(pyrrolidin-1-ylmethyl)-5-(trifluoromethyl)ph...)
Affinity DataIC50:  4nMpH: 7.2 T: 2°CAssay Description:Compounds were diluted into assay buffer containing Aurora kinase and FAM-PKAtide. The kinase reaction was initiated by adding ATP in assay buffer. T...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM50601172(CHEMBL5183104)
Affinity DataIC50:  4nMAssay Description:Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibito...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails PubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381810(US10272079, Compound 167)
Affinity DataIC50:  4.27nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381690(US10272079, Compound 47 | US10272079, Compound 66)
Affinity DataIC50:  4.47nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381789(US10272079, Compound 146)
Affinity DataIC50:  4.47nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381648(US10272079, Compound 6)
Affinity DataIC50:  4.47nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381690(US10272079, Compound 47 | US10272079, Compound 66)
Affinity DataIC50:  4.47nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetAurora kinase B(Homo sapiens (Human))
Sunesis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50310621(CHEMBL1079538 | N-(4-(6-(trifluoromethyl)-3H-imida...)
Affinity DataIC50:  5nMAssay Description:Inhibition of Aurora B after 60 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381739(US10272079, Compound 96)
Affinity DataIC50:  5.01nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381743(US10272079, Compound 100)
Affinity DataIC50:  5.01nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Homo sapiens (Human))
Ardelyx

Curated by ChEMBL
LigandPNGBDBM381678(US10272079, Compound 35)
Affinity DataIC50:  5.01nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetSodium/hydrogen exchanger 3(Rattus norvegicus)
Ardelyx

US Patent
LigandPNGBDBM381794(US10272079, Compound 151)
Affinity DataIC50:  5.01nMAssay Description:Cell-based activity under Prompt Conditions. Rat or human NHE3-mediated Na+-dependent H+ antiport was measured using a modification of the pH sensiti...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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