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Found 378 with Last Name = 'mccleland' and Initial = 'b'
TargetMuscarinic acetylcholine receptor M3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267614(4-[Hydroxy(diphenyl)methyl]-1-{2-[(phenylmethyl)ox...)
Affinity DataKi:  0.0600nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetMuscarinic acetylcholine receptor M3(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267573(4-[Hydroxy(diphenyl)methyl]-1-[3-(phenyloxy)propyl...)
Affinity DataKi:  0.130nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M3 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267614(4-[Hydroxy(diphenyl)methyl]-1-{2-[(phenylmethyl)ox...)
Affinity DataKi:  0.150nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M2 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267614(4-[Hydroxy(diphenyl)methyl]-1-{2-[(phenylmethyl)ox...)
Affinity DataKi:  0.160nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M1 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M1(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267573(4-[Hydroxy(diphenyl)methyl]-1-[3-(phenyloxy)propyl...)
Affinity DataKi:  0.640nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M1 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMuscarinic acetylcholine receptor M2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50267573(4-[Hydroxy(diphenyl)methyl]-1-[3-(phenyloxy)propyl...)
Affinity DataKi:  0.940nMAssay Description:Displacement of [3H]N-methyl scopalamine from human cloned muscarinic M2 receptor expressed in CHO cells coexpressing Gqi5 by scintillation proximity...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50125265(CHEMBL204021 | N-(2-Diethylamino-ethyl)-2-[2-(4-fl...)
Affinity DataIC50:  0.0490nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair
LigandPNGBDBM50521182(CHEMBL4456312 | US11260049, Ex. 123)
Affinity DataIC50:  0.300nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521192(CHEMBL4547537 | US11260049, Ex. 121)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521183(CHEMBL4461475 | US11260049, Ex. 125)
Affinity DataIC50:  0.5nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521183(CHEMBL4461475 | US11260049, Ex. 125)
Affinity DataIC50:  1nMAssay Description:Antagonist activity at rat TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50182422(CHEMBL3818650)
Affinity DataIC50:  1.40nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair
LigandPNGBDBM50502640(CHEMBL4470585)
Affinity DataIC50:  1.80nMAssay Description:Antagonist activity at human TRPV4More data for this Ligand-Target Pair
LigandPNGBDBM50521185(CHEMBL4439448 | US11260049, Ex. 83)
Affinity DataIC50:  2nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521195(CHEMBL4586959 | US11260049, Ex. 84)
Affinity DataIC50:  2nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 1(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50417996(CHEMBL1672434)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant cathepsin C after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50418002(CHEMBL1672427)
Affinity DataIC50:  2nMAssay Description:Inhibition of human recombinant cathepsin K after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50182421(CHEMBL3817896)
Affinity DataIC50:  2.40nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50505550(CHEMBL4439190 | US11260049, Ex. 2)
Affinity DataIC50:  3.20nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50505550(CHEMBL4439190 | US11260049, Ex. 2)
Affinity DataIC50:  3.20nMAssay Description:Antagonist activity at human TRPV4More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521186(CHEMBL4547101 | US11260049, Ex. 45)
Affinity DataIC50:  3.20nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50505551(CHEMBL4517101)
Affinity DataIC50:  3.5nMAssay Description:Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50182420(CHEMBL3819600)
Affinity DataIC50:  3.60nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50505543(CHEMBL4454801)
Affinity DataIC50:  3.80nMAssay Description:Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50505550(CHEMBL4439190 | US11260049, Ex. 2)
Affinity DataIC50:  4nMAssay Description:Antagonist activity at rat TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10 m...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50521180(CHEMBL4437115 | US11260049, Ex. 1)
Affinity DataIC50:  5nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50140791(1-(3-Bromo-4-cyano-2-hydroxy-phenyl)-3-(2-bromo-ph...)
Affinity DataIC50:  6nMAssay Description:Inhibition of binding of IL-8 to membranes of cloned CXC chemokine receptor 2 expressed in CHO Cells using [125I]-IL-8 radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50152761(3-[3-(2-Bromo-phenyl)-ureido]-6-chloro-2-hydroxy-b...)
Affinity DataIC50:  7nMAssay Description:Concentration required to inhibit [125I]IL-8 binding towards C-X-C chemokine receptor type 2 of human expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50521184(CHEMBL4476783)
Affinity DataIC50:  7.5nMAssay Description:Antagonist activity at TRPV4 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50505546(CHEMBL4533534 | US11260049, Ex. 82)
Affinity DataIC50:  7.90nMAssay Description:Antagonist activity at human TRPV4 expressed in HEK cells assessed as inhibition of GSK634775-induced calcium immobilization pre-incubated for 10 min...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCathepsin K(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50417991(CHEMBL1672425)
Affinity DataIC50:  7.94nMAssay Description:Inhibition of human recombinant cathepsin K after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 1(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50417991(CHEMBL1672425)
Affinity DataIC50:  7.94nMAssay Description:Inhibition of human recombinant cathepsin C after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203016(6-chloro-3-(3,4-dioxo-2-(phenylamino)cyclobut-1-en...)
Affinity DataIC50:  8nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50505546(CHEMBL4533534 | US11260049, Ex. 82)
Affinity DataIC50:  8nMAssay Description:Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203030(3-[4-chloro-3-(4-ethyl-piperazine-1-sulfonyl)-2-hy...)
Affinity DataIC50:  8nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50182419(CHEMBL3819444)
Affinity DataIC50:  9.5nMAssay Description:Inhibition of human recombinant Lp-PLA2 using 2-thio-PAF as substrate after 20 mins by CPM-based fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetDipeptidyl peptidase 1(Homo sapiens (Human))
TBA

Curated by ChEMBL
LigandPNGBDBM50417998(CHEMBL1672426)
Affinity DataIC50:  10nMAssay Description:Inhibition of human recombinant cathepsin C after 1 hrMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203007(3-(2-bromophenylamino)-4-(4-chloro-2-hydroxy-3-(4-...)
Affinity DataIC50:  10nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50152759(3-[3-(2-Bromo-phenyl)-ureido]-6-chloro-2-hydroxy-b...)
Affinity DataIC50:  10nMAssay Description:Concentration required to inhibit [125I]IL-8 binding towards C-X-C chemokine receptor type 2 of human expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50152760(3-[3-(2-Bromo-phenyl)-ureido]-6-chloro-2-hydroxy-N...)
Affinity DataIC50:  12nMAssay Description:Concentration required to inhibit [125I]IL-8 binding towards C-X-C chemokine receptor type 2 of human expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50505544(CHEMBL4550510)
Affinity DataIC50:  12nMAssay Description:Antagonist activity at BacMam virus expressing human TRPV4 transduced in BHK/AC9 or HEK MSR2 cells assessed as inhibition of GSK634775-induced Ca2+ f...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203035(3-(2-bromo-phenylamino)-4-[4-fluoro-2-hydroxy-3-(4...)
Affinity DataIC50:  13nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203036(6-chloro-3-(3,4-dioxo-2-(phenylamino)cyclobut-1-en...)
Affinity DataIC50:  14nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203028(3-(2-(o-toluidino)-3,4-dioxocyclobut-1-enylamino)-...)
Affinity DataIC50:  15nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203003(4-(2-(2-bromophenylamino)-3,4-dioxocyclobut-1-enyl...)
Affinity DataIC50:  15nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50187002(4-(3,4-dioxo-2-(phenylamino)cyclobut-1-enylamino)-...)
Affinity DataIC50:  15nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203003(4-(2-(2-bromophenylamino)-3,4-dioxocyclobut-1-enyl...)
Affinity DataIC50:  15nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203006(3-(4-chloro-2-hydroxy-3-(4-(piperidin-1-yl)piperid...)
Affinity DataIC50:  18nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPlatelet-activating factor acetylhydrolase(Homo sapiens (Human))
Astex Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM50182422(CHEMBL3818650)
Affinity DataIC50:  18nMAssay Description:Inhibition of Lp-PLA2 in human whole plasma using 2-thio-PAF as substrate preincubated for 15 mins followed by substrate addition measured after 3 mi...More data for this Ligand-Target Pair
TargetC-X-C chemokine receptor type 2(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50203025(3-(4-chloro-2-hydroxy-3-(4-methyl-1,4-diazepan-1-y...)
Affinity DataIC50:  20nMAssay Description:Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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