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Found 293 with Last Name = 'appell' and Initial = 'kc'
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254456(CHEMBL447392 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  11nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254457(CHEMBL443207 | N-(2-chlorobenzyl)-2-(N-(3-chloro-4...)
Affinity DataKi:  21nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254458(CHEMBL452238 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  34nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254456(CHEMBL447392 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  37nMAssay Description:Antagonist activity at human cloned B1 receptor expressed in african green monkey COS7 cells by calcium mobilization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254459(CHEMBL512111 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  93nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254460(CHEMBL499999 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  113nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254461(CHEMBL507546 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  149nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254457(CHEMBL443207 | N-(2-chlorobenzyl)-2-(N-(3-chloro-4...)
Affinity DataKi:  188nMAssay Description:Antagonist activity at human cloned B1 receptor expressed in african green monkey COS7 cells by calcium mobilization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254462(CHEMBL468492 | N-(2-methoxyphenethyl)-2-(N-(2-(ben...)
Affinity DataKi:  210nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254458(CHEMBL452238 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  267nMAssay Description:Antagonist activity at human cloned B1 receptor expressed in african green monkey COS7 cells by calcium mobilization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254463(3-(2-(2,4-dichloro-N-(2-(2,3-dihydro-1H-inden-5-yl...)
Affinity DataKi:  410nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254461(CHEMBL507546 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  463nMAssay Description:Antagonist activity at human cloned B1 receptor expressed in african green monkey COS7 cells by calcium mobilization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254459(CHEMBL512111 | N-(2-chlorobenzyl)-2-(N-(4-isobutox...)
Affinity DataKi:  497nMAssay Description:Antagonist activity at human cloned B1 receptor expressed in african green monkey COS7 cells by calcium mobilization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254508(3-(2-(2,4-dichloro-N-(2-(3-chlorophenoxy)ethyl)phe...)
Affinity DataKi:  1.09E+3nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254632(2-(2,4-dichloro-N-(2-(2,3-dihydro-1H-inden-5-yloxy...)
Affinity DataKi:  1.21E+3nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254633(3-(2-(N-(2-(benzo[d][1,3]dioxol-5-yloxy)ethyl)-2,4...)
Affinity DataKi:  1.57E+3nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254634(2-(2,4-dichloro-N-(2-(2,3-dihydro-1H-inden-5-yloxy...)
Affinity DataKi:  2.20E+3nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetB1 bradykinin receptor(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50254635(3-(2-(2,4-dichloro-N-(2-phenoxyethyl)phenylsulfona...)
Affinity DataKi:  1.30E+4nMAssay Description:Displacement of [3H]desArg from human B1 in human WI 38 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSubstance-P receptor(Rattus norvegicus (rat))
Rochester

Curated by ChEMBL
LigandPNGBDBM50009228(CHEMBL413846 | SP (substance P) | Spantide)
Affinity DataIC50:  0.120nMAssay Description:Binding affinity for tachykinin receptor 1 from rat forebrain tissue, [125I]-BH-SP as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSubstance-P receptor(Rattus norvegicus (rat))
Rochester

Curated by ChEMBL
LigandPNGBDBM50001450((SP)Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH...)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of Tachykinin receptor 1 of rat forebrain tissueMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSubstance-P receptor(Rattus norvegicus (rat))
Rochester

Curated by ChEMBL
LigandPNGBDBM50001450((SP)Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH...)
Affinity DataIC50:  0.120nMAssay Description:Inhibition of [125]I-Bolton Hunter Substance P([125]I-BHSP) binding to standard Tachykinin receptor 1 from rat forebrain membranes.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311657(1-(9-(8-fluorochroman-4-yl)-8-oxo-8,9-dihydro-7H-p...)
Affinity DataIC50:  1nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-V(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50277112(3-[1-Oxo-6-(1,2,3,4-tetrahydro-benzo[4,5]imidazo[1...)
Affinity DataIC50:  1nMAssay Description:Binding affinity to human integrin alphavbeta3 receptor by TRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50208999((R)-1-(2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-...)
Affinity DataIC50:  1.5nMAssay Description:Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-V(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50277111(3-Benzo[1,3]dioxol-5-yl-3-[1-oxo-6-(1,2,3,4-tetrah...)
Affinity DataIC50:  2nMAssay Description:Binding affinity to human integrin alphavbeta3 receptor by TRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325723((R)-2-(4-(4-chlorobenzyl)-5-methyl-4H-1,2,4-triazo...)
Affinity DataIC50:  2.90nMAssay Description:Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311656(2-(6-fluoro-1H-benzo[d]imidazol-1-yl)-9-(8-fluoroc...)
Affinity DataIC50:  3nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325722((R)-2-(4-(4-chlorobenzyl)-4H-1,2,4-triazol-3-yl)-N...)
Affinity DataIC50:  4nMAssay Description:Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK2(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311657(1-(9-(8-fluorochroman-4-yl)-8-oxo-8,9-dihydro-7H-p...)
Affinity DataIC50:  5nMAssay Description:Inhibition of human JAK2 (532-1132) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-V(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50277112(3-[1-Oxo-6-(1,2,3,4-tetrahydro-benzo[4,5]imidazo[1...)
Affinity DataIC50:  5nMAssay Description:Binding affinity to human integrin alphavbeta5 receptor by TRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50208999((R)-1-(2-(2-(4-(4-fluorobenzyl)-2-methylpiperazin-...)
Affinity DataIC50:  5.5nMAssay Description:Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50293055((R)-N2-(4-Chlorobenzyl)-N1-[2,6-dimethyl-4-(triflu...)
Affinity DataIC50:  6nMAssay Description:Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311644(1-(9-(2,6-difluorobenzyl)-8-oxo-8,9-dihydro-7H-pur...)
Affinity DataIC50:  6nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325719((R)-2-(1-(4-chlorobenzyl)-1H-tetrazol-5-yl)-N-(4-(...)
Affinity DataIC50:  6.5nMAssay Description:Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311640(1-(8-oxo-9-(tetrahydro-2H-pyran-4-yl)-8,9-dihydro-...)
Affinity DataIC50:  7nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-V(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50277098(3-[1-Oxo-6-(1,2,3,4-tetrahydro-benzo[4,5]imidazo[1...)
Affinity DataIC50:  7nMAssay Description:Binding affinity to human integrin alphavbeta3 receptor by TRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50293055((R)-N2-(4-Chlorobenzyl)-N1-[2,6-dimethyl-4-(triflu...)
Affinity DataIC50:  11nMAssay Description:Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311639(2-(6-chloro-1H-benzo[d]imidazol-1-yl)-9-(tetrahydr...)
Affinity DataIC50:  14nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetIntegrin alpha-V(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50277111(3-Benzo[1,3]dioxol-5-yl-3-[1-oxo-6-(1,2,3,4-tetrah...)
Affinity DataIC50:  14nMAssay Description:Binding affinity to human integrin alphavbeta5 receptor by TRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311655(2-(6-chloro-1H-benzo[d]imidazol-1-yl)-9-(8-fluoroc...)
Affinity DataIC50:  15nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50293054((R)-N2-(4-Chlorobenzyl)-N2-methyl-N1-[2-methyl-4-(...)
Affinity DataIC50:  16nMAssay Description:Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325718(2-(1-(4-chlorobenzyl)-1H-imidazol-2-yl)-N-(4-(trif...)
Affinity DataIC50:  16nMAssay Description:Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325722((R)-2-(4-(4-chlorobenzyl)-4H-1,2,4-triazol-3-yl)-N...)
Affinity DataIC50:  17nMAssay Description:Displacement of [125I]-MIP1alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetTyrosine-protein kinase JAK3(Homo sapiens (Human))
Ligand Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50311642(1-(9-(2,3-difluorobenzyl)-8-oxo-8,9-dihydro-7H-pur...)
Affinity DataIC50:  17nMAssay Description:Inhibition of human JAK3 (508-1124) by time resolved fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50413094(CHEMBL486116)
Affinity DataIC50:  18.6nMAssay Description:Antagonist activity at human OX2 receptor expressed in HEK293 cells assessed as inhibition of human orexin-A-stimulated calcium release by FLIPR assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetOrexin receptor type 2(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50413093(CHEMBL528990)
Affinity DataIC50:  19.5nMAssay Description:Antagonist activity at human OX2 receptor expressed in HEK293 cells assessed as inhibition of human orexin-A-stimulated calcium release by FLIPR assa...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325719((R)-2-(1-(4-chlorobenzyl)-1H-tetrazol-5-yl)-N-(4-(...)
Affinity DataIC50:  20nMAssay Description:Displacement of [125I]-MIP1alpha from human recombinant CCR1 expressed in HEK293 cells after 4 hrs by SPAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 3(Homo sapiens (Human))
Pharmacopeia Drug Discovery

Curated by ChEMBL
LigandPNGBDBM50175173(4-(4-((2,4-dichlorophenethyl)carbamoyl)-2-(3-chlor...)
Affinity DataIC50:  20nMAssay Description:Inhibition of CXCL10(IP-10)-stimulated calcium release in HEK293 cells expressing recombinant human CXCR3 and chimeric G protein Gqi5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50325720((R)-2-(1-(4-chlorobenzyl)-1H-1,2,4-triazol-5-yl)-N...)
Affinity DataIC50:  22nMAssay Description:Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL3-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-C chemokine receptor type 1(Homo sapiens (Human))
Pharmacopeia

Curated by ChEMBL
LigandPNGBDBM50293053((R)-N2-(4-Chlorobenzyl)-N1-[2-fluoro-4-(trifluorom...)
Affinity DataIC50:  22nMAssay Description:Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 3 hrsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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