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Found 386 with Last Name = 'pero' and Initial = 'je'
TargetCytochrome P450 3A4(Homo sapiens (Human))
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM50169690(CHEMBL3806137)
Affinity DataKi:  540nMAssay Description:Time dependent inhibition of CYP3A4 in human liver microsomesMore 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
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50240277(CHEMBL4061793)
Affinity DataIC50:  0.0600nMAssay Description:Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50240278(CHEMBL4062780)
Affinity DataIC50:  0.0900nMAssay Description:Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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
LigandPNGBDBM50502640(CHEMBL4470585)
Affinity DataIC50:  2nMAssay Description:Antagonist activity at human TRPV4More data for this Ligand-Target Pair
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 TRPV4More 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 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
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
TargetSodium channel protein type 8 subunit alpha(Homo sapiens (Human))
Merck

Curated by ChEMBL
LigandPNGBDBM50240282(CHEMBL4090731)
Affinity DataIC50:  4.70nMAssay Description:Inhibition of human Nav1.6 alpha expressed in HEK293 cells incubated for 5 mins with 6 consecutive train pulses to -10 mV at 0.1 Hz and holding poten...More data for this Ligand-Target Pair
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
LigandPNGBDBM50521180(CHEMBL4437115 | US11260049, Ex. 1)
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
LigandPNGBDBM50505550(CHEMBL4439190 | US11260049, Ex. 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
LigandPNGBDBM539865(4-(((3S,4S)-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
LigandPNGBDBM539874(4-(((3S,4R)-1- ((2-chloro-4- fluorophenyl)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
LigandPNGBDBM539875(4-(((3S,4R)-1- ((2-chloro-4- methylphenyl)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
LigandPNGBDBM539876(2-chloro-4-(difluoro- methyl)benzene-1- sulfonyl c...)
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
LigandPNGBDBM539872(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
LigandPNGBDBM539878(4-chloro-2- methoxybenzene- 1-sulfonyl chloride | ...)
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
LigandPNGBDBM539879(5-chloro-2- (((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
LigandPNGBDBM539916(3-chloro-4- (((3R,4S)-3- hydroxy-3- (hydroxymethyl...)
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
LigandPNGBDBM539917(3- (difluoromethyl)- 4-(((3R,4S)-3- hydroxy-3- (hy...)
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
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
LigandPNGBDBM539936(4-(((3R,4S)-4-((4-bromophenyl)sulfonyl)-3-hydroxy-...)
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
LigandPNGBDBM539937(4-(((3S,4S)-1- ((2,4- dichlorophenyl) sulfonyl)-4-...)
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
LigandPNGBDBM50505546(CHEMBL4533534 | US11260049, Ex. 82)
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
LigandPNGBDBM50521185(CHEMBL4439448 | US11260049, Ex. 83)
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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