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Found 2901 with Last Name = 'aki' and Initial = 'c'
TargetDimer of Gag-Pol polyprotein [489-587](Human immunodeficiency virus type 1)
Boehringer Ingelheim Pharmaceuticals

LigandPNGBDBM729((2S,4R)-N-tert-butyl-1-[(2R,3S)-2-hydroxy-3-[(2S)-...)
Affinity DataKi:  0.0310nM ΔG°:  -62.4kJ/mole IC50:  4nMpH: 5.5 T: 2°CAssay Description:Sensitivity of HIV-1 protease activity to protease inhibitors was determined by a peptide substrate cleavage assay. Cleavage products and substrate w...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataKi:  0.0530nMAssay Description:Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50241203(CHEMBL414357 | HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGS...)
Affinity DataKi:  0.0920nMAssay Description:Displacement of [125I]GLP-1 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetDimer of Gag-Pol polyprotein [514-612](Human immunodeficiency virus type 2)
Boehringer Ingelheim Pharmaceuticals

LigandPNGBDBM729((2S,4R)-N-tert-butyl-1-[(2R,3S)-2-hydroxy-3-[(2S)-...)
Affinity DataKi:  0.130nM ΔG°:  -58.7kJ/mole IC50:  10nMpH: 5.5 T: 2°CAssay Description:Sensitivity of HIV-1 protease activity to protease inhibitors was determined by a peptide substrate cleavage assay. Cleavage products and substrate w...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50086603(CHEMBL3426241)
Affinity DataKi:  0.570nMAssay Description:Displacement of [125I]-17 from human GLP-1R expressed in CHO cell membranes incubated for 120 mins by scintillation counting based radioligand bindin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211457(3-(2-((R)-1-(4-sec-butylfuran-2-yl)propylamino)-3,...)
Affinity DataKi:  0.600nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50301953((3S,6S,9S,12S,15S,21S)-21-(2-((S)-2-amino-3-(1H-im...)
Affinity DataKi:  0.660nMAssay Description:Displacement of [125I]-17 from human GLP-1R expressed in CHO cell membranes incubated for 120 mins by scintillation counting based radioligand bindin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin D(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50080960(2-Bromo-N-[(1S,2S)-3-{[2-(2,4-dichloro-phenyl)-eth...)
Affinity DataKi:  0.700nMAssay Description:Inhibition of cathepsin D (unknown origin)More data for this Ligand-Target Pair
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211449((R)-3-(3,4-dioxo-2-(1-(4-(pentan-3-yl)furan-2-yl)p...)
Affinity DataKi:  0.800nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211454((R)-3-(2-(1-(4-ethylfuran-2-yl)propylamino)-3,4-di...)
Affinity DataKi:  1nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211458((R)-2-hydroxy-3-(2-(1-(4-isopropylfuran-2-yl)propy...)
Affinity DataKi:  1nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetUDP-3-O-acyl-N-acetylglucosamine deacetylase(Escherichia coli)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50200120(CHEMBL260091 | CHIR-090 | US10875832, Compound ChI...)
Affinity DataKi:  2nMAssay Description:Inhibition of Escherichia coli LpxCMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211453((R)-3-(2-(1-(4-butylfuran-2-yl)propylamino)-3,4-di...)
Affinity DataKi:  2nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211456((R)-2-hydroxy-3-(2-(1-(4-isopropylfuran-2-yl)ethyl...)
Affinity DataKi:  2nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211450((R)-3-(2-(1-(4-cyclopentylfuran-2-yl)propylamino)-...)
Affinity DataKi:  3nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211458((R)-2-hydroxy-3-(2-(1-(4-isopropylfuran-2-yl)propy...)
Affinity DataKi:  3nMAssay Description:Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211462((R)-3-(2-(cyclopropyl(4-isopropylfuran-2-yl)methyl...)
Affinity DataKi:  3nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50297764((R)-5-cyano-3-(3,4-dioxo-2-(1-phenylpropylamino)cy...)
Affinity DataKi:  3nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAromatase(Homo sapiens (Human))
Tohoku Pharmaceutical University

LigandPNGBDBM9989((2S,6S,15S)-6-hydroxy-2-(hydroxymethyl)-15-methylt...)
Affinity DataKi:  3.40nM ΔG°:  -50.3kJ/mole IC50:  31nMpH: 7.5 T: 2°CAssay Description:The enzyme activity was assayed by measuring the 3H-labeled H2O formed from [1beta-3H] Androstenedione during aromatization. After incubation, the re...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211464((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(4-methylfuran-...)
Affinity DataKi:  4nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211452((R)-2-hydroxy-3-(2-(1-(4-isopropylfuran-2-yl)-2-me...)
Affinity DataKi:  4nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50297761((R)-6-bromo-3-(3,4-dioxo-2-(1-phenylpropylamino)cy...)
Affinity DataKi:  4nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211459((R)-3-(2-(1-(4-cyclohexylfuran-2-yl)propylamino)-3...)
Affinity DataKi:  4nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211455((R)-3-(2-(1-(4-tert-butylfuran-2-yl)propylamino)-3...)
Affinity DataKi:  4nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211448((R)-2-hydroxy-3-(2-(1-(4-isopropylfuran-2-yl)-2,2-...)
Affinity DataKi:  4nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50240819(CHEMBL4084119)
Affinity DataKi:  4.40nMAssay Description:Displacement of [125I]GLP-1 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50236053((R)-3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobut-1...)
Affinity DataKi:  4.40nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50297740((R)-3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobut-1...)
Affinity DataKi:  4.5nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211451((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(4-methylthioph...)
Affinity DataKi:  5nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50200877((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylthioph...)
Affinity DataKi:  5nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50200880((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylfuran-...)
Affinity DataKi:  5nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50250387(CHEMBL4102791)
Affinity DataKi:  5nMAssay Description:Displacement of [125I]-CXCL12 from human CXCR7 expressed in CHOK1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50297741((R)-5-cyano-3-(3,4-dioxo-2-(1-(thiophen-2-yl)propy...)
Affinity DataKi:  5nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50200880((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(5-methylfuran-...)
Affinity DataKi:  5nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50297738((R)-1-(3-(3,4-dioxo-2-(1-phenylpropylamino)cyclobu...)
Affinity DataKi:  5nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50200887((R)-3-(3,4-dioxo-2-(1-(thiophen-2-yl)propylamino)c...)
Affinity DataKi:  5nMAssay Description:Displacement of human [125I]IL-8 from human CXCR2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50250387(CHEMBL4102791)
Affinity DataKi:  5.01nMAssay Description:Displacement of [125I]-CXCL12 from human CXCR7 expressed in CHOK1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAromatase(Homo sapiens (Human))
Tohoku Pharmaceutical University

LigandPNGBDBM9997((2S,15S)-2-(hydroxymethyl)-15-methyltetracyclo[8.7...)
Affinity DataKi:  5.80nM ΔG°:  -48.9kJ/mole IC50:  49nMpH: 7.5 T: 2°CAssay Description:The enzyme activity was assayed by measuring the 3H-labeled H2O formed from [1beta-3H] Androstenedione during aromatization. After incubation, the re...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAromatase(Homo sapiens (Human))
Tohoku Pharmaceutical University

LigandPNGBDBM9994((2R,8R,15S)-8-hydroxy-2,15-dimethyltetracyclo[8.7....)
Affinity DataKi:  6nM ΔG°:  -48.8kJ/mole IC50:  50nMpH: 7.5 T: 2°CAssay Description:The enzyme activity was assayed by measuring the 3H-labeled H2O formed from [1beta-3H] Androstenedione during aromatization. After incubation, the re...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211463((S)-3-(3,4-dioxo-2-(2,2,2-trifluoro-1-(4-isopropyl...)
Affinity DataKi:  6nMAssay Description:Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50086602(CHEMBL3426300)
Affinity DataKi:  6nMAssay Description:Displacement of [125I]-17 from human GLP-1R expressed in CHO cell membranes incubated for 120 mins by scintillation counting based radioligand bindin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucagon-like peptide 1 receptor(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50240819(CHEMBL4084119)
Affinity DataKi:  6.30nMAssay Description:Displacement of [3H]PF-06883365 from FAP-tagged human GLP-1R expressed in CHO cells assessed as inhibition constant by radioligand binding assayMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetAromatase(Homo sapiens (Human))
Tohoku Pharmaceutical University

LigandPNGBDBM9996((2R,15S)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{...)
Affinity DataKi:  6.80nM ΔG°:  -48.5kJ/mole IC50:  60nMpH: 7.5 T: 2°CAssay Description:The enzyme activity was assayed by measuring the 3H-labeled H2O formed from [1beta-3H] Androstenedione during aromatization. After incubation, the re...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211454((R)-3-(2-(1-(4-ethylfuran-2-yl)propylamino)-3,4-di...)
Affinity DataKi:  7nMAssay Description:Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211457(3-(2-((R)-1-(4-sec-butylfuran-2-yl)propylamino)-3,...)
Affinity DataKi:  7.60nMAssay Description:Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50250402(CHEMBL4084835)
Affinity DataKi:  7.90nMAssay Description:Displacement of [125I]-CXCL12 from human CXCR7 expressed in CHOK1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50264278(CHEMBL4064803)
Affinity DataKi:  7.90nMAssay Description:Displacement of [125I]CXCL12 from human CXCR7 expressed in CHO-K1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50264278(CHEMBL4064803)
Affinity DataKi:  7.94nMAssay Description:Displacement of [125I]CXCL12 from human CXCR7 expressed in CHO-K1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetAtypical chemokine receptor 3(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50250402(CHEMBL4084835)
Affinity DataKi:  8nMAssay Description:Displacement of [125I]-CXCL12 from human CXCR7 expressed in CHOK1 cell membranes after 2 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 1(Homo sapiens (Human))
Schering-Plough Research Institute

Curated by ChEMBL
LigandPNGBDBM50211464((R)-2-hydroxy-N,N-dimethyl-3-(2-(1-(4-methylfuran-...)
Affinity DataKi:  9nMAssay Description:Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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