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Found 401 with Last Name = 'brnardic' and Initial = 'ej'
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12133(3-(Indol-2-yl)indazole 23 | [5-(3-{5-[(4-fluoropip...)
Affinity DataIC50:  0.110nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12134(2-methoxy-4-{3-[5-(piperidin-1-ylmethyl)-1H-indol-...)
Affinity DataIC50:  0.25nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12131((5-{3-[5-(piperidin-1-ylmethyl)-1H-indol-2-yl]-1H-...)
Affinity DataIC50:  0.300nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12132(3-(Indol-2-yl)indazole 22 | [5-(3-{5-[(4-fluoropip...)
Affinity DataIC50:  0.300nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More data for this Ligand-Target Pair
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
LigandPNGBDBM50450513(CHEMBL4168219)
Affinity DataIC50:  1nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 or HEK MSR2 cells assessed as inhibition of PF-04674114-induced Ca2+ flux pre-incubated for 1...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM50220886(5-(3-aminopropyl)-7,8-dicyclohexyl-3-methyl-2H-pyr...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of Chk1 by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM92404(CHEMBL250843 | PDK1 inhibitor, 5)
Affinity DataIC50:  1.20nMAssay Description:Inhibition of Chk1 by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50022671(CHEMBL3298265)
Affinity DataIC50:  1.5nMAssay Description:Inhibition of purified TrkA cytoplasmic domain (unknown origin) by HTRF assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12112(1-[4-({2-[6-(1H-1,2,3,4-tetrazol-5-yl)-1H-indazol-...)
Affinity DataIC50:  2.30nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
LigandPNGBDBM50450500(CHEMBL4164465)
Affinity DataIC50:  2.5nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 or HEK MSR2 cells assessed as inhibition of PF-04674114-induced Ca2+ flux pre-incubated for 1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
LigandPNGBDBM50450500(CHEMBL4164465)
Affinity DataIC50:  2.5nMAssay Description:Antagonist activity at human TRPV4 expressed in BHK/AC9 or HEK MSR2 cells assessed as inhibition of PF-04674114-induced Ca2+ flux pre-incubated for 1...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM12126(3-(Indol-2-yl)indazole 16 | 3-[5-(piperidin-1-ylme...)
Affinity DataIC50:  2.60nMpH: 7.5 T: 2°CAssay Description:Kinase activity was measured in a homogeneous assay in a 96-well format. Detection was performed by HTRF using an EuK-labelled anti-phospho(S21)-GSK3...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHigh affinity nerve growth factor receptor(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50446392(CHEMBL3109645 | US9181261, 2)
Affinity DataIC50:  3nMAssay Description:Inhibition of human TrkA expressed in human U2OS cells assessed as inhibition of NGF-induced maximum response after 1 hr by beta-galactosidase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM50220898((R)-5-(3-amino-2-fluoropropyl)-7,8-dicyclohexyl-3-...)
Affinity DataIC50:  3.10nMAssay Description:Inhibition of Chk1 by 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 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
TargetSerine/threonine-protein kinase Chk1(Homo sapiens (Human))
Merck Research Laboratories

LigandPNGBDBM50220884((S)-5-(3-amino-2-fluoropropyl)-7,8-dicyclohexyl-3-...)
Affinity DataIC50:  3.20nMAssay Description:Inhibition of Chk1 by 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
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
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
LigandPNGBDBM50450503(CHEMBL3218118)
Affinity DataIC50:  4nMAssay Description:Antagonist activity at TRPV4 (unknown origin)More data for this Ligand-Target Pair
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
LigandPNGBDBM436106(4-(((3S,4S)-4-(aminomethyl)-1-((5-chloropyridin-2-...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539921(4-(((3S,4R)-1- ((2-bromo-4- chlorophenyl)sulfonyl)...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539896(4-(((3S,4R)-1- ((4-bromo-2- chlorophenyl)sulfonyl)...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539897(4-(((3R,4S)-4- ((4-chloro- phenyl)sulfonyl)- 3-hyd...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539900(3-bromo-4- (((3R,4S)-4-((4- chlorophenyl)sulfonyl)...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50521186(CHEMBL4547101 | US11260049, Ex. 45)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539910(4-(((3R,4S)-4- ((4-chloro- phenyl)sulfonyl)- 3-hyd...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM436099(4-(((3S,4R)-1-((2,4-dichlorophenyl)sulfonyl)-4-hyd...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM436104(4-(((3S,4R)-1- ((2-cyano-4- (trifluoromethyl) phen...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM436105(4-(((3S,4R)-1- ((2-chloro-4- cyanophenyl) sulfonyl...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539969(3-chloro-4- (((3R,4S)-4-((4- chloro-3- fluoropheny...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539975(4-(((3R,4S)-4-((5- bromopyridin-2- yl)sulfonyl)-3-...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539979(2-(((3R,4S)-4-((4- chlorophenyl) sulfonyl)-3- hydr...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539981(3-chloro-4-(((3R,4S)-4-((5-chloropyridin-2-yl)sulf...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539982(3-chloro-4-(((3R,4S)-4-((5-chloropyridin-2-yl)sulf...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50521192(CHEMBL4547537 | US11260049, Ex. 121)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539984(4-(((3R,4S)-3- (aminomethyl)-4- ((4-chlorophenyl) ...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50521182(CHEMBL4456312 | US11260049, Ex. 123)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539986(3-chloro-4- (((3S,4S)-4-((4- chlorophenyl) sulfony...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM50521183(CHEMBL4461475 | US11260049, Ex. 125)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
LigandPNGBDBM539932(4-(((3S,4R)-1- ((4-cyano-2-methyl- phenyl)sulfonyl...)
Affinity DataIC50:  5nMAssay Description:TRPV4 channel activation results in an influx of divalent and monovalent cations including calcium. The resulting changes in intracellular calcium we...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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