Query String: Treg-mediated suppression
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- ChEMBL_860170 (CHEMBL2168711) Inhibition of human recombinant CatB assessed as suppression of enzyme-mediated Z-Arg-Arg-AMC cleavage by QFRET assay
- ChEMBL_860171 (CHEMBL2168712) Inhibition of dog recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage by QFRET assay
- ChEMBL_1673723 (CHEMBL4023752) Inhibition of BTK in human whole blood derived-basophils assessed as suppression of IgE mediated-FcepsilonR ligation-stimulated CD63 expression
- ChEMBL_860169 (CHEMBL2168710) Inhibition of human recombinant CatS assessed as suppression of enzyme-mediated Z-Val-Val-Arg-AMC cleavage by QFRET assay
- ChEMBL_860167 (CHEMBL2168708) Inhibition of human recombinant CatK assessed as suppression of enzyme-mediated Z-Phe-Arg-AMC cleavage incubated for 1 hrs by QFRET assay
- ChEMBL_1526512 (CHEMBL3635400) Inhibition of porcupine activity (unknown origin) expressed in human HT1080 cells assessed as suppression of Wnt3A-mediated super top flash activity by STF luciferase assay
- ChEMBL_1929752 (CHEMBL4432928) Activation of p75NTR in C57BL/6 mouse brain assessed as suppression of carbachol-mediated persistant firing of entorhinal cortex after 15 mins by current-clamp technique
- ChEMBL_1996564 (CHEMBL4630459) Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
- ChEMBL_1996565 (CHEMBL4630460) Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
- ChEMBL_1561408 (CHEMBL3778968) Antagonist activity at human CB2 receptor transfected in CHO cells assessed as inhibition of WIN 55,212-2 mediated suppression of forksolin induced cAMP production by scintillation counting analysis
- ChEMBL_28877 (CHEMBL645947) AP-1 suppression activity using freshly prepared DMSO stock
- ChEMBL_1755230 (CHEMBL4189990) Antagonist activity at P2Y14R in rat C6 cells assessed as suppression of UDP-glucose-mediated inhibition of forskolin-stimulated [3H]cyclic-AMP accumulation after 15 mins in presence of [3H]-adenine
- ChEMBL_2078172 (CHEMBL4733963) Inhibition of NAE (unknown origin)-mediated neddylation assessed as suppression of cullin1-Nedd8 adduct formation preincubated for 10 mins followed by ATP addition and measured after 30 mins by immunoblot analysis
- ChEMBL_1647802 (CHEMBL3996858) Inhibition of PI3Kdelta in mouse spleen assessed suppression of CD86
- ChEMBL_28878 (CHEMBL645948) AP-1 suppression activity using one month old DMSO stock
- ChEMBL_28879 (CHEMBL645949) AP-1 suppression activity using one week old DMSO stock
- ChEMBL_28880 (CHEMBL645950) AP-1 suppression activity using six months old DMSO stock
- ChEMBL_28881 (CHEMBL645951) AP-1 suppression activity using two months old DMSO stock
- ChEMBL_1575938 (CHEMBL3802561) Antagonist activity at human adenosine A1 receptor expressed in CHO cell membranes assessed as suppression of CCPA-mediated inhibition of cAMP level by scintillation counting method in presence of [3H]-cyclic AMP
- ChEMBL_1866231 (CHEMBL4367206) Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
- ChEMBL_2339693 Inhibition of PRMT5 in human Z138 cells assessed as suppression of sDMA level
- ChEMBL_862992 (CHEMBL2175172) Inhibition of STAT3 assessed as suppression of STAT3-DNA interaction by EMSA
- ChEMBL_1625597 (CHEMBL3868066) Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth
- ChEMBL_1625599 (CHEMBL3868068) Inhibition of JAK3 in mouse HT2 cells assessed as suppression of cell growth
- ChEMBL_1719139 (CHEMBL4134139) Inhibition of PI3Kdelta in human whole blood assessed as suppression of CD69 expression
- ChEMBL_1571690 (CHEMBL3795721) Antagonist activity against EP4 in human whole blood assessed as reversal of PGE2-mediated suppression of LPS-induced TNF-alpha production preincubated for 30 mins followed by LPS stimulation measured after 20 to 24 hrs by enzyme immunoassay
- ChEMBL_1476877 (CHEMBL3429911) Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
- ChEMBL_1615834 (CHEMBL3857903) Inhibition of serotonin transporter (unknown origin) assessed as suppression of synaptosomal uptake of serotonin
- ChEMBL_1615835 (CHEMBL3857904) Inhibition of norepinephrine transporter (unknown origin) assessed as suppression of synaptosomal uptake of norepinephrine
- ChEMBL_1615836 (CHEMBL3857905) Inhibition of dopamine transporter (unknown origin) assessed as suppression of synaptosomal uptake of dopamine
- ChEMBL_1838911 (CHEMBL4339044) Inhibition of TGFbetaR1 in anti-CD3/anti-CD28/IL-2/TGFbeta -stimulated human Treg cells assessed as downregulation of FOXP3 expression incubated for 5 days by flow cytometry analysis
- ChEBML_32651 Inhibition of alphaV-beta3 mediated cell adhesion
- ChEMBL_2491993 Inhibition of CXCL12 (unknown origin) mediated chemotaxis
- ChEMBL_378652 (CHEMBL871488) Inhibition of COX1-mediated platelet aggregation
- ChEMBL_464100 (CHEMBL948141) Inhibition of NET mediated norepinephrine uptake
- ChEMBL_620187 (CHEMBL1115822) Inhibition of PTP1B mediated pNPP hydrolysis
- ChEMBL_806012 (CHEMBL1960448) Inhibition of rat DAT-mediated uptake
- ChEMBL_806014 (CHEMBL1960450) Inhibition of rat NET-mediated uptake
- ChEMBL_806084 (CHEMBL1960687) Inhibition of rat SERT-mediated uptake
- ChEMBL_810619 (CHEMBL2015670) Inhibition of Lyp-mediated pNPP hydrolysis
- ChEMBL_819963 (CHEMBL2032550) Inhibition of CCR2-mediated calcium mobilization
- ChEMBL_819964 (CHEMBL2032551) Inhibition of CCR2-mediated Erk phosphorylation
- ChEMBL_84043 (CHEMBL691889) Inhibition HCV NS5B-mediated RNA synthesis
- ChEMBL_861794 (CHEMBL2173387) Inhibition of SYK-mediated PLCgamma phosphorylation
- ChEMBL_861795 (CHEMBL2173388) Inhibition of SYK-mediated LAT phosphorylation
- ChEMBL_1567367 (CHEMBL3789507) Inhibition of EGFR L858R mutant in human H3255 cells assessed as suppression of cell proliferation
- ChEMBL_1985558 (CHEMBL4618964) Inverse agonist activity at RORgammat in mouse whole blood assessed as suppression of Th17 secretion
- ChEBML_217620 Inhibition of alpha4-beta7 integrin mediated cell adhesion
- ChEBML_217630 Inhibition of alpha5-beta1 integrin mediated cell adhesion
- ChEBML_67350 Ability to activate estrogen receptor 1-mediated transcription.
- ChEMBL_1367904 Inhibition of DAT (unknown origin)-mediated dopamine reuptake
- ChEMBL_1367905 Induction of SERT (unknown origin)-mediated serotonin release
- ChEMBL_1767545 (CHEMBL4219657) Inhibition of DAT (unknown origin)-mediated uptake
- ChEMBL_1767546 (CHEMBL4219658) Inhibition of NET (unknown origin)-mediated uptake
- ChEMBL_1767568 (CHEMBL4219680) Inhibition of SERT (unknown origin)-mediated uptake
- ChEMBL_2297921 Inhibition of RAD51 (unknown origin) mediated homologous recombination
- ChEMBL_2310738 Inhibition of recombinant human CTSL-mediated substrate cleavage
- ChEMBL_2354280 Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux
- ChEMBL_32646 (CHEMBL642141) Inhibition of alphaL-beta2 mediated cell adhesion
- ChEMBL_334421 (CHEMBL862502) Inhibition of LTB4 mediated human eosinophil chemotaxis
- ChEMBL_334422 (CHEMBL862503) Inhibition of C5a mediated human eosinophil chemotaxis
- ChEMBL_334423 (CHEMBL862504) Inhibition of PAF mediated human eosinophil chemotaxis
- ChEMBL_350561 (CHEMBL868994) Inhibition of TARC-mediated CEM cell migration
- ChEMBL_432312 (CHEMBL915572) Inhibition of HIV1 integrase-mediated integration activity
- ChEMBL_464099 (CHEMBL948140) Inhibition of SERT mediated 5-hydroxytryptamine uptake
- ChEMBL_465478 (CHEMBL933182) Inhibition of topoisomerase 1-mediated DNA relaxation
- ChEMBL_465479 (CHEMBL933183) Inhibition of topoisomerase 2 mediated DNA relaxation
- ChEMBL_467033 (CHEMBL932723) Inhibition of MIF-mediated dopachrome tautomerase activity
- ChEMBL_467083 (CHEMBL934766) Inhibition of stromelysin mediated beta-casein cleavage
- ChEMBL_473556 (CHEMBL939226) Inhibition of p56lck-mediated exogenous peptide phosphorylation
- ChEMBL_473707 (CHEMBL936806) Inhibition of Chk1 mediated phosphorylation of cdc25C
- ChEMBL_485096 (CHEMBL1013206) Inhibition of cathepsin B mediated osteoporotic activity
- ChEMBL_546026 (CHEMBL1034201) Inhibition of Cdc7-mediated phosphorylation of Mcm2
- ChEMBL_643969 (CHEMBL1211868) Inhibition of human CYP3A4-mediated midazolam oxidation
- ChEMBL_643970 (CHEMBL1211869) Inhibition of human CYP3A4-mediated testosterone oxidation
- ChEMBL_745635 (CHEMBL1776005) Inhibition of human GAT1-mediated GABA uptake
- ChEMBL_745637 (CHEMBL1776007) Inhibition of rat GAT2-mediated GABA uptake
- ChEMBL_745638 (CHEMBL1776008) Inhibition of human GAT3-mediated GABA uptake
- ChEMBL_749801 (CHEMBL1787961) Inhibition of NHE1-mediated rat platelet swelling
- ChEMBL_802794 (CHEMBL1953528) Inhibition of human CCR2-mediated Erk phosphorylation
- ChEMBL_807237 (CHEMBL1960167) Inhibition of rat DAT-mediated dopamine reuptake
- ChEMBL_807238 (CHEMBL1960168) Inhibition of rat NET-mediated norepinephrine reuptake
- ChEMBL_807239 (CHEMBL1960169) Inhibition of rat SERT-mediated serotonin reuptake
- ChEMBL_824329 (CHEMBL2044471) Inhibition of rat DAT-mediated dopamine reuptake
- ChEMBL_824331 (CHEMBL2044473) Inhibition of rat NET-mediated norepinephrine reuptake
- ChEMBL_824333 (CHEMBL2044475) Inhibition of rat SERT-mediated serotonin reuptake
- ChEMBL_873346 (CHEMBL2185199) Inhibition of CYP3A4-mediated midazolam 1'-hydroxylation
- ChEBML_1686221 Inhibition of BTK in goat F(ab')2anti-mouse IgM-stimulated Balb/c mouse splenocyte B cells assessed as suppression of BCR-mediated CD86 induction preincubated for 60 mins followed by cell stimulation measured after 24 hrs by 7AAD staining-based FACS analysis
- ChEBML_195788 In vitro inhibitory activity against human plasma renin at pH 5.5 for suppression of angiotensin I formation.
- ChEMBL_1474783 (CHEMBL3424240) Induction of p53-dependent growth suppression of human LNZTA3 cells after 72 hrs by MTT assay
- ChEMBL_1567368 (CHEMBL3789508) Inhibition of EGFR Del ex19 mutant in human HCC827 cells assessed as suppression of cell proliferation
- ChEMBL_1567369 (CHEMBL3789747) Inhibition of EGFR Del ex19 mutant in human PC9 cells assessed as suppression of cell proliferation
- ChEMBL_1567373 (CHEMBL3789751) Inhibition of wild type EGFR in human NCI-H1666 cells assessed as suppression of cell proliferation
- ChEMBL_1616866 (CHEMBL3858935) Inhibition of LCK in human peripheral T cells assessed as suppression of TCR-dependant cell proliferation
- ChEMBL_1719734 (CHEMBL4134734) Inhibition of NADPH-reduced rat TrxR1 assessed as suppression of DTNB reduction incubated for 1 hr
- ChEMBL_537437 (CHEMBL990602) Antagonist activity at TLR4 in human PBMC cells assessed as suppression of LPS-induced cytokine upregulation
- ChEMBL_542877 (CHEMBL1010700) Transrepression activity at GR in human SW1353 cells assessed as suppression of NFkappaB-induced IL8 production
- ChEMBL_1707419 (CHEMBL4058652) Inhibition of CBP in human PBMC derived naive CD4-positive T cells assessed as decrease in FOXP3 mRNA level in Treg cells measured after 4 days by quantitative reverse transcriptase-PCR method
- ChEMBL_1446327 (CHEMBL3374293) Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production
- ChEMBL_1616864 (CHEMBL3858933) Inhibition of BTK in human PBM cells assessed as suppression of FCRgammaR/immune complex-stimulated TNFalpha production
- ChEMBL_1628556 (CHEMBL3871141) Inhibition of tyrosinase in human MNT1 cells assessed as suppression of melanin biosynthesis measured after 96 hrs
- ChEMBL_1647794 (CHEMBL3996850) Inhibition of PI3Kdelta in human whole blood assessed as suppression of CD69 expression incubated for 60 mins
- ChEBML_35865 Antithrombin III (ATIII)-mediated anti-Xa activity was determined
- ChEMBL_1295089 (CHEMBL3129464) Inhibition of smoothened (unknown origin)-mediated Shh signaling
- ChEMBL_1335757 (CHEMBL3239787) Inhibition of BRAF (unknown origin)-mediated ERK phosphorylation
- ChEMBL_1339909 (CHEMBL3243746) Inhibition of human NEP-mediated amyloid beta hydrolysis
- ChEMBL_1339911 (CHEMBL3243748) Inhibition of human ACE-mediated amyloid beta hydrolysis
- ChEMBL_1367803 Inhibition of DAT-mediated dopamine uptake in rat synaptosomes
- ChEMBL_1367804 Induction of DAT-mediated dopamine release in rat synaptosomes
- ChEMBL_1367805 Inhibition of SERT-mediated serotonin uptake in rat synaptosomes
- ChEMBL_1367806 Induction of SERT-mediated serotonin release in rat synaptosomes
- ChEMBL_1547438 (CHEMBL3757557) Inhibition of ASCT2 (unknown origin)-mediated glutamine transport
- ChEMBL_162548 (CHEMBL768535) In vitro inhibition of PKC mediated DNA cleavage.
- ChEMBL_2224724 (CHEMBL5138237) Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation
- ChEMBL_2285414 Inhibition of P-gp (unknown origin) mediated ATP hydrolysis
- ChEMBL_2310748 Inhibition of SARS-CoV-1 RdRp-mediated viral replication
- ChEMBL_30118 (CHEMBL640475) Inhibition of alphaIIb-beta3 integrin mediated platelet aggregation
- ChEMBL_310318 (CHEMBL833274) Effective concentration for DP2 mediated chemotaxis in eosinophils
- ChEMBL_334424 (CHEMBL862505) Inhibition of Eotaxin mediated by human eosinophil chemotaxis
- ChEMBL_432311 (CHEMBL915571) Inhibition of HIV1 integrase-mediated 3'-processing activity
- ChEMBL_438660 (CHEMBL888991) Inhibition of IP10-induced CXCR3 mediated cell migration
- ChEMBL_438661 (CHEMBL888992) Inhibition of ITAC-induced CXCR3 mediated cell migration
- ChEMBL_438662 (CHEMBL888993) Inhibition of MIG-induced CXCR3 mediated cell migration
- ChEMBL_453902 (CHEMBL885906) Inhibition of recombinant HIV1 integrase mediated-disintegration activity
- ChEMBL_595215 (CHEMBL1040871) Inhibition of human CES2-mediated pNPA substrate turnover
- ChEMBL_616146 (CHEMBL1103009) Inhibition of HSP90-mediated client protein HER2 degradation
- ChEMBL_639378 (CHEMBL1167758) Inhibition of Mycobacterium tuberculosis PTPA-mediated pNPP hydrolysis
- ChEMBL_67350 (CHEMBL676806) Ability to activate estrogen receptor 1-mediated transcription.
- ChEMBL_67671 (CHEMBL673864) Ability to activate estrogen receptor 2-mediated transcription.
- ChEMBL_700342 (CHEMBL1647668) Inhibition of MCP1-mediated human THP cell migration
- ChEMBL_90715 (CHEMBL702114) Inhibition of HIV-1 integrase-mediated 3'-processing
- ChEMBL_90716 (CHEMBL701109) Inhibition of HIV-1 integrase-mediated strand transfer
- ChEMBL_929798 (CHEMBL3068773) Inhibition of DUSP26 (unknown origin)-mediated p38 dephosphorylation
- ChEMBL_941896 (CHEMBL2329962) Inhibition of MMP7 (unknown origin)-mediated omniMMP degradation
- ChEMBL_941897 (CHEMBL2329963) Inhibition of human recombinant IDE-mediated insulin degradation
- ChEMBL_941899 (CHEMBL2329965) Inhibition of human recombinant IDE-mediated FRET1 degradation
- ChEMBL_976022 (CHEMBL2415671) Inhibition of human recombinant PTP1B-mediated pNPP hydrolysis
- ChEMBL_976625 (CHEMBL2416957) Inhibition of RIP1/JNK2 (unknown origin)-mediated necrosis
- ChEMBL_990647 (CHEMBL2447658) Inhibition of rat ROMK channel-mediated 86Rb+ flux
- ChEMBL_1446342 (CHEMBL3374308) Agonist activity at GR in mouse RAW cells assessed as suppression of TNF-alpha-induced IL-6 production
- ChEMBL_1567255 (CHEMBL3788712) Activation of GPR109A in human A431 cells assessed as suppression of forskolin-induced cAMP production after 30 mins
- ChEMBL_1567366 (CHEMBL3789506) Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation
- ChEMBL_1567370 (CHEMBL3789748) Inhibition of EGFR Del ex19/T790M double mutant in human PC9 cells assessed as suppression of cell proliferation
- ChEMBL_1570710 (CHEMBL3795078) Inhibition of gamma-secretase (unknown origin) assessed as suppression of amyloid beta 42 production by cell-based assay
- ChEMBL_1570813 (CHEMBL3795240) Inhibition of gamma-secretase (unknown origin) assessed as suppression of amyloid beta 40 production by cell-based assay
- ChEMBL_1616863 (CHEMBL3858932) Inhibition of BTK in human peripheral B cells assessed as suppression of CD40/CD40L-stimulated CD69 surface expression
- ChEMBL_1891419 (CHEMBL4393246) Inhibition of Cav3.2 (unknown origin) assessed as suppression of KCl-evoked current by whole-cell patch clamp method
- ChEMBL_1926332 (CHEMBL4429404) Inhibition of BTK in human peripheral B cells assessed as suppression of CD40/CD40L stimulated CD69 surface expression
- ChEMBL_560040 (CHEMBL1021560) Agonist activity at human CB2 receptor expressed in CHO cells assessed as suppression of forskolin-stimulated cAMP accumulation
- ChEMBL_560042 (CHEMBL1022429) Agonist activity at human CB1 receptor expressed in CHO cells assessed as suppression of forskolin-stimulated cAMP accumulation
- ChEBML_202616 Inhibition of Src-mediated dentine resorption in rabbit-osteoclast assay
- ChEMBL_1289619 (CHEMBL3118126) Inhibition of human wild-type ALDH3A1-mediated benzaldehyde oxidation
- ChEMBL_1335300 (CHEMBL3238724) Inhibition of AChE (unknown origin)-mediated amyloid beta aggregation
- ChEMBL_1336707 (CHEMBL3240855) Inhibition of CRTH2 receptor-mediated chemotaxis in human basophils
- ChEMBL_1824910 (CHEMBL4324674) Inhibition of CXCR2-mediated chemotaxis in mouse BAF3 cells
- ChEMBL_1925268 (CHEMBL4428340) Inhibition of gamma secretase (unknown origin) mediated Notch signaling
- ChEMBL_1925288 (CHEMBL4428360) Inhibition of gamma secretase (unknown origin) mediated Notch activation
- ChEMBL_2104670 (CHEMBL4813173) Inhibition of Nav1.5 (unknown origin)-mediated late channel current
- ChEMBL_30128 (CHEMBL641170) Inhibition of alpha IIb beta III mediated platelet aggregation
- ChEMBL_302763 (CHEMBL838827) Inhibition of glucocorticoid receptor mediated tyrosine amino transferase activity
- ChEMBL_312574 (CHEMBL835240) Inhibition of alphaIIb-beta3 integrin mediated platelet aggregation (PLAGGIN15)
- ChEMBL_329077 (CHEMBL863001) Inhibition of CXCL11-induced CXCR3 mediated T-cell migration
- ChEMBL_384427 (CHEMBL866710) Inhibition of EGFR-mediated polyGAT phosphorylation at 10 uM
- ChEMBL_423294 (CHEMBL855465) Inhibition of P-selectin-mediated adhesion of HL60 cells
- ChEMBL_440752 (CHEMBL889849) Inhibition of gamma secretase-mediated amyloid-beta peptid aggregation
- ChEMBL_458969 (CHEMBL925063) Inhibition of HIV1 integrase-mediated 3'-end processing activity
- ChEMBL_469851 (CHEMBL949039) Inhibition of MK2-mediated HSP27 phosphorylation in THP1 cells
- ChEMBL_479892 (CHEMBL935745) Inhibition of rat brain FAAH mediated [14C]anandamide hydrolysis
- ChEMBL_491804 (CHEMBL945194) Inhibition of p38alpha-mediated TNFalpha production in peripheral mononucleocytes
- ChEMBL_50468 (CHEMBL658171) Inhibition of the gyrase mediated cleavage of supercoiled DNA
- ChEMBL_508741 (CHEMBL1004035) Inhibition of HIV1 RT mediated DNA-dependent DNA polymerization
- ChEMBL_54529 (CHEMBL663875) Inhibitory activity against topo II-mediated decatenation of DNA
- ChEMBL_547439 (CHEMBL1029254) Inhibition of sheep placental cotyledons COX2-mediated prostaglandin production
- ChEMBL_571090 (CHEMBL816916) Inhibition of MMP1-mediated collagen degradation by SDS-PAGE
- ChEMBL_571091 (CHEMBL816917) Inhibition of MMP13-mediated collagen degradation by SDS-PAGE
- ChEMBL_578280 (CHEMBL1053101) Inhibition of SYK-mediated inhibition of biotinylated substrate phosphorylation
- ChEMBL_578285 (CHEMBL1053842) Inhibition of Zap70-mediated inhibition of biotinylated substrate phosphorylation
- ChEMBL_578286 (CHEMBL1053843) Inhibition of MK2-mediated inhibition of biotinylated substrate phosphorylation
- ChEMBL_578287 (CHEMBL1053844) Inhibition of LCK-mediated inhibition of biotinylated substrate phosphorylation
- ChEMBL_599194 (CHEMBL1049837) Inhibition of COX1-mediated PGH2 production by enzyme immunoassay
- ChEMBL_599195 (CHEMBL1049838) Inhibition of COX2-mediated PGH2 production by enzyme immunoassay
- ChEMBL_603789 (CHEMBL1042927) Inhibition of integrin alpha5beta1 receptor-mediated HEK293 cell adhesion
- ChEMBL_618631 (CHEMBL1101519) Inhibition of deoxycytidine kinase-mediated arabinoside C-induced cytotoxicity
- ChEMBL_619310 (CHEMBL1099474) Inhibition of human FAAH-mediated hydrolysis of [3H]AEA
- ChEMBL_641537 (CHEMBL1175371) Inhibition of human ACC1/2-mediated malonyl-CoA synthesis
- ChEMBL_653502 (CHEMBL1226705) Inhibition of Rad3-related (ATR) protein-mediated p53 phosphorylation
- ChEMBL_695427 (CHEMBL1639097) Inhibition of recombinant ATX mediated hydrolysis of FS-3
- ChEMBL_795885 (CHEMBL1936449) Inhibition of ACAT1- mediated cholesteryl ester synthesis in macrophages
- ChEMBL_858231 (CHEMBL2167858) Reversible inhibition of mouse UT-B-mediated urea transport
- ChEMBL_884439 (CHEMBL2212201) Inhibition of CRTH2 receptor-mediated chemotaxis in human basophils
- ChEMBL_884723 (CHEMBL2215604) Inhibition of B-Raf V600E mutant -mediated MEK phosphorylation
- ChEMBL_90265 (CHEMBL699130) Inhibition of insulin receptor mediated mitogenesis of NIH3T3 cells
- ChEMBL_962568 (CHEMBL2390763) Inhibition of human GSK3beta-mediated YRRAAVPPSPSLSRHSSPHQ(pS)EDEEE phosphorylation
- ChEMBL_1616861 (CHEMBL3858930) Inhibition of BTK in human peripheral B cells assessed as suppression of BCR/anti-IgM/IgG-stimulated cell proliferation
- ChEMBL_1616868 (CHEMBL3858937) Inhibition of BTK in human whole blood basophils assessed as suppression of FceRI/anti-IgE-stimulated CD63 surface expression
- ChEMBL_1926330 (CHEMBL4429402) Inhibition of BTK in human tonsillar B cells assessed as suppression of BCR/anti-IgM/IgG stimulated cell proliferation
- ChEMBL_2124448 (CHEMBL4833681) Inhibition of EZH2 in human U2932 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2124449 (CHEMBL4833682) Inhibition of EZH2 in human Raji cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2124450 (CHEMBL4833683) Inhibition of EZH2 in human Daudi cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEBML_144902 Antagonism of batrachotoxin-mediated sodium ion uptake into cultured neuroblastoma cells
- ChEBML_146451 In vitro opioid receptor delta mediated mouse vas deferens (MVD) assay
- ChEBML_90196 In vitro inhibition of ADP-mediated human gel filtered platelet aggregation.
- ChEMBL_1344246 (CHEMBL3256076) Inhibition of NET-mediated norepinephrine uptake in rat brain synaptosomes
- ChEMBL_1748556 (CHEMBL4183066) Inhibition of CYP3A4-mediated midazolam metabolism in human liver microsomes
- ChEMBL_1748557 (CHEMBL4183067) Inhibition of CYP3A4-mediated testosterone metabolism in human liver microsomes
- ChEMBL_1980356 (CHEMBL4613618) Inhibition of calf thymus gland topoisomerase 1 mediated DNA relaxation
- ChEMBL_2112526 (CHEMBL4821376) Inhibition of ABCC1 mediated etoposide resistant in human 2008 cells
- ChEMBL_212172 (CHEMBL819020) Inhibitory activity against trypsin mediated Tyr-Gly-Aer-p- nitroaniline
- ChEMBL_2281003 Inhibition of rat SULT2A1-mediated dehydroepiandrosterone sulfonation incubated for 20 mins
- ChEMBL_2285336 Inhibition of FTO (unknown origin) mediated m6A methylation by HPLC analysis
- ChEMBL_2433665 Inhibition of LasR-mediated quorum sensing system in Pseudomonas aeruginosa PAO1
- ChEMBL_2444652 Inhibition of SOS1 (unknown origin) mediated KRAS activation by HTRF method
- ChEMBL_30123 (CHEMBL640480) Inhibition of alpha IIb beta-3 integrin mediated platelet aggregation
- ChEMBL_30127 (CHEMBL641169) Inhibition of alpha IIb beta-3 integrin mediated platelet aggregation
- ChEMBL_305758 (CHEMBL829529) Inhibitory concentration against HIV-1 integrase mediated 3' processing reaction
- ChEMBL_305788 (CHEMBL827976) Inhibitory concentration against HIV-1 integrase mediated strand transfer reaction
- ChEMBL_312773 (CHEMBL835185) Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activity
- ChEMBL_372237 (CHEMBL853390) Inhibition of DAT-mediated [3H]DA uptake in rat striatum
- ChEMBL_376176 (CHEMBL869312) Inhibition of rat NET-mediated norepinephrine uptake in CHO cells
- ChEMBL_376177 (CHEMBL869313) Inhibition of rat SERT-mediated serotonin uptake in CHO cells
- ChEMBL_376306 (CHEMBL867962) Activity at human FPRL1-mediated calcium mobilization in CHO cells
- ChEMBL_419414 (CHEMBL913014) Inhibition of LFA1-mediated adhesion of T cell to HUVEC
- ChEMBL_422232 (CHEMBL856485) Inhibition of PKA-mediated phosphorylation of kemptide at 100 uM
- ChEMBL_447306 (CHEMBL896339) Inhibition of recombinant CHK-mediated Cdc25C phosphorylation after 30 mins
- ChEMBL_455659 (CHEMBL886442) Inhibition of BACE1-mediated sAPP-NF processing in HEK293 cells
- ChEMBL_461817 (CHEMBL928946) Antagonist activity at CXCR3 assessed as ITAC-mediated cell migration
- ChEMBL_461818 (CHEMBL928947) Antagonist activity at CXCR3 assessed as MIG-mediated cell migration
- ChEMBL_475725 (CHEMBL934611) Inhibition of human recombinant p38alpha-mediated myelin basic protein phosphorylation
- ChEMBL_477689 (CHEMBL925845) Inhibition of human URAT1-mediated urate uptake in HEK293 cells
- ChEMBL_491805 (CHEMBL945195) Inhibition of p38alpha-mediated IL1-beta production in peripheral mononucleocytes
- ChEMBL_492345 (CHEMBL948341) Inhibition of recombinant TK1-mediated phosphorylation of [CH3-3H]deoxythymidine
- ChEMBL_499799 (CHEMBL972431) Inhibition of Gli1-mediated transcription expressed in human PANC1 cells
- ChEMBL_499800 (CHEMBL972432) Inhibition of Gli2-mediated transcription expressed in human PANC1 cells
- ChEMBL_537435 (CHEMBL990600) Inhibition of TLR2-mediated IL8 secretion in human THP1 cells
- ChEMBL_537439 (CHEMBL990604) Inhibition of human TLR4-mediated cytokine production in mouse macrophages
- ChEMBL_547440 (CHEMBL1029255) Inhibition of bovine seminal vesicle microsomal COX1-mediated prostaglandin production
- ChEMBL_557786 (CHEMBL953295) Inhibition of MAGL-mediated 2-arachidonoylglycerol hydrolysis in mouse brain
- ChEMBL_557788 (CHEMBL953297) Inhibition of FAAH-mediated [3H]anandamide hydrolysis in mouse brain
- ChEMBL_571759 (CHEMBL1033004) Inhibition of rat recombinant FAAH-mediated hydrolysis of [3H]AEA
- ChEMBL_577794 (CHEMBL1054721) Inhibition of FAAH-mediated anandamide hydrolysis in rat brain membrane
- ChEMBL_595431 (CHEMBL1040072) Inhibition of p38alpha-mediated ATF2 phosphorylation in presence of ATP
- ChEMBL_615170 (CHEMBL1106955) Inhibition of GRK1-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615171 (CHEMBL1106956) Inhibition of GRK2-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615172 (CHEMBL1106957) Inhibition of GRK3-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615173 (CHEMBL1106958) Inhibition of GRK4-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615174 (CHEMBL1106959) Inhibition of GRK5-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615175 (CHEMBL1106960) Inhibition of GRK6-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_615176 (CHEMBL1106961) Inhibition of GRK7-mediated bovine tubulin phosphorylation by scintillation counting
- ChEMBL_621465 (CHEMBL1100026) Inhibition of human recombinant CYP3A4-mediated oxidation of 7-benzyloxyquinoline
- ChEMBL_634323 (CHEMBL1120736) Inhibition of SERT-mediated serotonin uptake in human JAR cells
- ChEMBL_654585 (CHEMBL1243629) Inhibition of human IGF1R-mediated Poly Glu4Tyr phosphorylation by ELISA
- ChEMBL_675467 (CHEMBL1273604) Inhibition of PAR1-mediated aggregation of TRAP-stimulated human platelet
- ChEMBL_686691 (CHEMBL1290871) Inhibition of CETP-mediated neutral lipid transfer by fluorometric analysis
- ChEMBL_741476 (CHEMBL1763791) Inhibition of AKT1-mediated PRAS40 phosphorylation in human LNCaP cells
- ChEMBL_754945 (CHEMBL1805767) Inhibition of nicotinamide phosphoribosyltransferase-mediated decrease in cellular NAD level
- ChEMBL_789248 (CHEMBL1924373) Inhibition of human IKK2-mediated GST-IkappaBalpha protein fusion phosphorylation
- ChEMBL_79534 (CHEMBL691015) HEK cell adhesion mediated by alpha v beta 3 integrin
- ChEMBL_795467 (CHEMBL1937472) Inhibition of CETP-mediated neutral lipid transfer by fluorometric analysis
- ChEMBL_797435 (CHEMBL1943098) Inhibition of DGAT1-mediated triglyceride synthesis n mouse 3T3L1 cells
- ChEMBL_797474 (CHEMBL1943217) Inhibition of MK2-mediated HSP27 phosphorylation by cell-based assay
- ChEMBL_801201 (CHEMBL1949072) Inhibition of mTOR-mediated S6 phosphorylation in human PC3 cells
- ChEMBL_801202 (CHEMBL1949073) Inhibition of mTOR-mediated Akt phosphorylation in human PC3 cells
- ChEMBL_809512 (CHEMBL2015429) Inhibition of human SERT-mediated serotonin reuptake in HEK293 cells
- ChEMBL_822969 (CHEMBL2038290) Inhibition of DGAT1-mediated triacylglycerol synthesis in human HuTu80 cells
- ChEMBL_828304 (CHEMBL2050323) Inhibition of histamine H4 receptor-mediated chemotaxis in human eosinophils
- ChEMBL_862854 (CHEMBL2172956) Inhibition of GST tagged PERK cytoplasmic domain mediated EIF2alpha phosphorylation
- ChEMBL_873338 (CHEMBL2185191) Inhibition of CYP3A4-mediated N-demethylation in human liver microsomes
- ChEMBL_948337 (CHEMBL2341171) Inhibition of CYP1A2 (unknown origin)-mediated phenaceten demethylation to acetaminophen
- ChEMBL_1457064 (CHEMBL3369185) Inverse agonist activity at human RoRc in human skin model assessed as suppression of IL-17A level relative to control
- ChEMBL_1457926 (CHEMBL3370833) Inverse agonist activity at human RoRc in human skin model assessed as suppression of IL-17F level relative to control
- ChEMBL_1616862 (CHEMBL3858931) Inhibition of BTK in human peripheral B cells assessed as suppression of BCR/anti-IgM/IgG-stimulated CD86 surface expression
- ChEMBL_1616865 (CHEMBL3858934) Inhibition of ITK in human peripheral T cells assessed as suppression of TCR/anti-CD3-stimulated protein catalyzed PLCgamma1 phosphorylation
- ChEMBL_1622885 (CHEMBL3865237) Inhibition of PI3Kbeta in human PC3 cells assessed as suppression of AKT phosphorylation at Ser473 after 60 mins by ELISA
- ChEMBL_1622886 (CHEMBL3865238) Inhibition of PI3Kbeta in human PC3 cells assessed as suppression of AKT phosphorylation at Thr308 after 60 mins by ELISA
- ChEMBL_1926333 (CHEMBL4429405) Inhibition of BTK in human PBMC assessed as suppression of FCgamma2aR/FCgamma3R stimulated TNFalpha production after 7 hrs by ELISA
- ChEMBL_2339699 Inhibition of PRMT5 in human MCF7 cells assessed as suppression of arginine sDMA incubated for 3 days by target engagement assay
- ChEMBL_1572803 (CHEMBL3804527) Inhibition of FGFR1 in human H1581 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay
- ChEMBL_1572804 (CHEMBL3804528) Inhibition of FGFR1 in human KG1 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay
- ChEMBL_1572806 (CHEMBL3804530) Inhibition of FGFR3 in human RT112 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay
- ChEMBL_1613024 (CHEMBL3854824) Inhibition of CDK8 in human COLO205 cells expressing APC mutant assessed as suppression of WNT pathway by luciferase reporter gene assay
- ChEMBL_1613025 (CHEMBL3854825) Inhibition of CDK8 in human PA1 cells assessed as suppression of WNT3a ligand-induced WNT pathway by luciferase reporter gene assay
- ChEMBL_1647793 (CHEMBL3996849) Inhibition of PI3Kdelta in BCR-stimulated human B cells assessed as suppression of CD86 expression after 18 hrs by FACS analysis
- ChEMBL_1655315 (CHEMBL4004681) Inhibition of DOT1L in human MOLM13 cells assessed as suppression of HoxA9 gene after 72 hrs by luciferase reporter gene assay
- ChEMBL_1856573 (CHEMBL4357302) Inhibition of Listeria monocytogenes NAD kinase assessed as suppression of reduced NADP formation by yeast glucose-6-phosphate dehydrogenase coupled assay
- ChEMBL_1924917 (CHEMBL4427873) Inhibition of PI3Kdelta in BCR-stimulated human B cells assessed as suppression of CD86 expression after 18 hrs by FACS analysis
- ChEMBL_1934648 (CHEMBL4480300) Inhibition of DOT1L in human MOLM13 cells assessed as suppression of HoxA9 gene after 72 hrs by luciferase reporter gene assay
- ChEMBL_2046474 (CHEMBL4701173) Inhibition of BTK in human PBMC assessed as suppression of TNFalpha/FcgammaR-induced monocyte activation by measuring reduction in cytokine production
- ChEMBL_2124451 (CHEMBL4833684) Inhibition of EZH2 A677G mutant in human Pfeiffer cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2124452 (CHEMBL4833685) Inhibition of EZH2 Y641F mutant in human WSUDLCL2 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2339658 Inhibition of PRMT5 in human Granta-519 cells assessed as suppression of sDMA level incubated for 3 days by western blot analysis
- ChEBML_215988 Inhibition of glycoprotein IIb/III integrin mediated fibrinogen binding to activated platelets
- ChEMBL_101651 (CHEMBL710307) Inhibitory concentration determined on an HIV infection model mediated by CXCR4
- ChEMBL_1335625 (CHEMBL3239512) Inhibition of JAK2 (unknown origin)-mediated STAT5 phosphorylation by AlphaScreen assay
- ChEMBL_1352340 (CHEMBL3269757) Inhibition of EPAC1 (unknown origin) assessed as cAMP-mediated GEF activity
- ChEMBL_1453579 (CHEMBL3363164) Inhibition of DAT (unknown origin) assessed as transporter-mediated dopamine reuptake
- ChEMBL_1460661 (CHEMBL3395902) Inhibition of JNK3-mediated c-jun phosphorylation in rat INS1 cells
- ChEMBL_1525160 (CHEMBL3635498) Inhibition of FKBP12 (unknown origin)-mediated rotamase activity by spectrophotometric analysis
- ChEMBL_162517 (CHEMBL766763) Activation of Purinoceptor P2Y1-mediated phospholipase C in turkey erythrocyte membranes
- ChEMBL_1772712 (CHEMBL4229704) Inhibition of C2-mediated MAC formation in human serum by ELISA
- ChEMBL_2108852 (CHEMBL4817527) Inhibition of ASM (unknown origin)-mediated KRAS mislocalization from plasma membrane
- ChEMBL_2226389 (CHEMBL5139902) Inhibition of SARS-CoV-2 papain-like protease-mediated de-ISGylation
- ChEMBL_2260011 (CHEMBL5215022) Inhibition of human CXCR2-mediated chemotaxis expressed in mouse BaF3 cells
- ChEMBL_2265572 Inhibition of mutant HTT (unknown origin) mediated HD exon 1 protein aggregation
- ChEMBL_2281002 Inhibition of rat liver SULT1A1-mediated oestradiol sulfonation incubated for 20 mins
- ChEMBL_2290233 Inhibition of GLI1-mediated transcriptional activity in human HaCaT cells coexpressing luciferase
- ChEMBL_2491987 Inhibition of 20s proteasome beta5 site (unknown origin) mediated chymotrypsin-like activity
- ChEMBL_305249 (CHEMBL833506) Concentration required for inhibition of HIV-1 integrase mediated strand transfer
- ChEMBL_310504 (CHEMBL833243) Effective concentration for DP2 mediated stimulation of actin polymerization in eosinophils
- ChEMBL_329115 (CHEMBL863431) Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR
- ChEMBL_359728 (CHEMBL869334) Inhibition of rat AR-mediated reporter gene expression in COS7 cells
- ChEMBL_372239 (CHEMBL853393) Inhibition of NET-mediated [3H]NE uptake in rat cerebral cortex
- ChEMBL_376175 (CHEMBL869308) Inhibition of rat DAT-mediated [3H]dopamine uptake in CHO cells
- ChEMBL_378454 (CHEMBL871028) Inhibition of FLAG-p66/HIS-p51-mediated HIV1 reverse transcriptase dimerization
- ChEMBL_421070 (CHEMBL854907) Inhibition of MCH-mediated calcium influx into MCH-R1 expressing cells
- ChEMBL_437153 (CHEMBL906550) Inhibition of SKca channel-mediated after-hypepolarization in rat sympathetic neurons
- ChEMBL_447424 (CHEMBL896442) Inhibition of gamma secretase-mediated beta amyloid production in NIH3T3 cells
- ChEMBL_461816 (CHEMBL928945) Antagonist activity at CXCR3 assessed as IP-10-mediated cell migration
- ChEMBL_466008 (CHEMBL948317) Inhibition of steroid sulfatase-mediated conversion of [3H]E1S to E1
- ChEMBL_473084 (CHEMBL921796) Inhibition of human COX2 mediated PGE2 production in human whole blood
- ChEMBL_484514 (CHEMBL1014040) Inhibition of xanthine oxidase-mediated formation of uric acid by spectrophotometry
- ChEMBL_506252 (CHEMBL942442) Inhibition of 5LO-mediated LTB4 production in human neutrophils by RIA
- ChEMBL_508986 (CHEMBL1005539) Inhibition of Tel-fused EphB4 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508987 (CHEMBL1005540) Inhibition of Tel-fused Tie2 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508988 (CHEMBL1005541) Inhibition of Tel-fused PDGFRb kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508989 (CHEMBL1005542) Inhibition of Tel-fused FLT3 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508991 (CHEMBL1005544) Inhibition of Tel-fused KDR kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508992 (CHEMBL1005545) Inhibition of Tel-fused FLT1 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508993 (CHEMBL1005546) Inhibition of Tel-fused FGFR1 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508994 (CHEMBL1005547) Inhibition of Tel-fused RET kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508995 (CHEMBL1006336) Inhibition of Tel-fused RON kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508996 (CHEMBL1006337) Inhibition of Tel-fused MET kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508997 (CHEMBL1006338) Inhibition of Tel-fused TRKB kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508998 (CHEMBL1006339) Inhibition of Tel-fused ALK kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_508999 (CHEMBL1006340) Inhibition of Tel-fused JAK2 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509000 (CHEMBL1006341) Inhibition of Tel-fused TYK2 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509001 (CHEMBL1006342) Inhibition of Tel-fused SRC kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509002 (CHEMBL1006343) Inhibition of Tel-fused Lyn kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509003 (CHEMBL1006344) Inhibition of Tel-fused Bmx kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509004 (CHEMBL1006345) Inhibition of Tel-fused Abl kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509005 (CHEMBL1006346) Inhibition of Tel-fused ZAP70 kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509006 (CHEMBL1006347) Inhibition of Tel-fused Syk kinase-mediated mouse BaF3 cell proliferation
- ChEMBL_509876 (CHEMBL998721) Inhibition of CYP2D6-mediated metabolism of dextromethorphan in human liver microsomes
- ChEMBL_537919 (CHEMBL982706) Inhibition of FAAH-mediated [14C]anandamide hydrolysis in rat brain membrane
- ChEMBL_54345 (CHEMBL669720) In vitro 50% inhibition of topoisomerase II mediated k-DNA decatenation
- ChEMBL_557787 (CHEMBL953296) Inhibition of MAGL-mediated [14C]1-oleoylglycerol hydrolysis in mouse brain
- ChEMBL_578976 (CHEMBL1061425) Inhibition of 5LOX-mediated LTB4 formation in stimulated human polymorphonuclear leukocytes
- ChEMBL_600206 (CHEMBL1046364) Inhibition of EGFR-mediated poly(L-glutamic acid L-tyrosine) phosphorylation
- ChEMBL_607766 (CHEMBL1068737) Inhibition of CBR-mediated NADPH-dependent reduction of menadione to menadiol
- ChEMBL_611777 (CHEMBL1066434) Noncompetitive inhibition of autotaxin-mediated FS3 hydrolysis by Michaelis-Menten analysis
- ChEMBL_634326 (CHEMBL1120739) Inhibition of human NET-mediated norepinephrine uptake in MDCK-Net6 cells
- ChEMBL_654092 (CHEMBL1228898) Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells
- ChEMBL_654586 (CHEMBL1243630) Inhibition of human insulin receptor-mediated Poly Glu4Tyr phosphorylation by ELISA
- ChEMBL_66886 (CHEMBL675510) Inhibition of Epidermal growth factor receptor mediated mitogenesis of NIH3T3 cells
- ChEMBL_695893 (CHEMBL1640945) Inhibition of recombinant MPO mediated taurine chlorination by microplate reader method
- ChEMBL_739728 (CHEMBL1763554) Inhibition of human EGFR-mediated poly(Glu4Tyr) phosphorylation after 1 hr
- ChEMBL_747761 (CHEMBL1780960) Inhibition of B-Raf-mediated ERK phosphorylation in cell-based assay
- ChEMBL_789632 (CHEMBL1924717) Inhibition of COX2-mediated PGE2 production in human whole blood assay
- ChEMBL_790354 (CHEMBL1925807) Inhibition of human topoisomerase 2alpha-mediated relaxation of supercoiled pBR322 DNA
- ChEMBL_790355 (CHEMBL1925808) Inhibition of human topoisomerase 1-mediated relaxation of supercoiled pBR322 DNA
- ChEMBL_807301 (CHEMBL1960394) Inhibition of GSK3beta-mediated CRMP-2 phosphorylation by cell based assay
- ChEMBL_819216 (CHEMBL2032485) Inhibition of recombinant c-met-mediated gastrin phosphorylation by HTRF assay
- ChEMBL_828101 (CHEMBL2049840) Inhibition of PKCtheta-mediated IL-2 production by cell based assay
- ChEMBL_830489 (CHEMBL2061259) Inhibition of human recombinant P38alpha-mediated ATF2 phosphorylation after 1 hr
- ChEMBL_840522 (CHEMBL2089873) Inhibition of JNK1-mediated ATF2 phosphorylation after 1 hr by ELISA
- ChEMBL_887592 (CHEMBL2217201) Inhibition of human thrombin-mediated platelet aggregation in cell-based assay
- ChEMBL_90023 (CHEMBL699522) Inhibition of ADP-mediated platelet aggregation in human gel-filtered platelets
- ChEMBL_939698 (CHEMBL2328923) Inhibition of recombinant SAE1(unknown origin)-mediated SUMOylation of RanGAP1-C2
- ChEMBL_948334 (CHEMBL2341168) Inhibition of CYP3A4 (unknown origin)-mediated midazolam hydroxylation to 1'-Hydroxymidazolam
- ChEMBL_948335 (CHEMBL2341169) Inhibition of CYP2D6 (unknown origin)-mediated bufuralol hydroxylation to 4'-Hydroxybufuralol
- ChEMBL_948336 (CHEMBL2341170) Inhibition of CYP2C9 (unknown origin)-mediated tolbutamide hydroxylation to hydroxy tolbutamide
- ChEMBL_96792 (CHEMBL703269) Inhibition of LFA-1 mediated HL60 cell adhesion to ICAM-1
- ChEMBL_987744 (CHEMBL2439835) Inhibition of 5-LOX (unknown origin)-mediated leukotriene (LT)B4 biosynthesis
- ChEMBL_991566 (CHEMBL2445311) Inhibition of estrogen receptor alpha-mediated human MCF7 cell growth inhibition
- ChEMBL_1929423 (CHEMBL4432599) Inhibition of Shh-N-induced Gli1 (unknown origin) expressed in mouse Shh Light2 cells assessed as Gli1-mediated mediated transcription incubated for 30 hrs by firefly luciferase assay
- ChEMBL_813150 (CHEMBL2020816) Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay
- ChEMBL_1572615 (CHEMBL3803148) Inhibition of recombinant FGFR2 in human SNU16 cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay
- ChEMBL_1572805 (CHEMBL3804529) Inhibition of FGFR2 in human KATO III cells assessed as suppression of cell proliferation after 72 hrs by SRB/CCK-8 assay
- ChEMBL_1585156 (CHEMBL3820804) Inhibition of recombinant rat GluN1a/GluN2A co-expressed in HEK293 cells assessed as suppression of glutamate-induced current by patch-clamp method
- ChEMBL_1585157 (CHEMBL3820805) Inhibition of recombinant rat GluN1a/GluN2B co-expressed in HEK293 cells assessed as suppression of glutamate-induced current by patch-clamp method
- ChEMBL_1585158 (CHEMBL3820806) Inhibition of recombinant rat GluN1a/GluN2C co-expressed in HEK293 cells assessed as suppression of glutamate-induced current by patch-clamp method
- ChEMBL_1613023 (CHEMBL3854823) Inhibition of CDK8 in human LS174T cells expressing beta-catenin mutant assessed as suppression of WNT pathway by luciferase reporter gene assay
- ChEMBL_1885969 (CHEMBL4387551) Inhibition of COX1 (unknown origin) assessed as suppression of PGG2 conversion to PGH2 incubated fro 2 mins by TMPD based colorimetric assay
- ChEMBL_1885970 (CHEMBL4387552) Inhibition of COX2 (unknown origin) assessed as suppression of PGG2 conversion to PGH2 incubated fro 2 mins by TMPD based colorimetric assay
- ChEMBL_1891418 (CHEMBL4393245) Inhibition of recombinant human Cav3.1 expressed in HEK293 cells assessed as suppression of KCl-evoked current by whole-cell patch clamp method
- ChEMBL_2048853 (CHEMBL4703552) Inhibition of LSD1 in human NCI-H69 cells assessed as suppression of GRP mRNA expression incubated for 4 days by qPCR analysis
- ChEMBL_2048854 (CHEMBL4703553) Inhibition of LSD1 in human NCI-H1417 cells assessed as suppression of GRP mRNA expression incubated for 4 days by qPCR analysis
- ChEMBL_2048855 (CHEMBL4703554) Inhibition of LSD1 in human NCI-H1417 cells assessed as suppression of GRP mRNA expression incubated for 12 days by qPCR analysis
- ChEMBL_2119984 (CHEMBL4829131) Inhibition of human AAK1 expressed in HEK293 cells assessed as suppression of AP2 phosphorylation measured after 3 hrs by Western blot analysis
- ChEMBL_2123074 (CHEMBL4832307) Inhibition of ErbB4 in human T47D cells assessed as suppression of neuregulin 1-induced autophosphorylation incubated for 90 mins by sandwich ELISA
- ChEMBL_2124453 (CHEMBL4833686) Inhibition of EZH2 Y641N mutant in human KARPAS-422 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2339657 Inhibition of PRMT5 in human U-87 MG cells assessed as suppression of sDMA level incubated for 3 days by western blot analysis
- ChEBML_208412 Inhibitory effect on topoisomerase-1 mediated DNA cleavage using supercoiled pBR322 plasmid DNA
- ChEBML_221964 In vitro activity against topoisomerase-1 mediated cleavage of supercoiled pBR322 plasmid DNA
- ChEBML_3968 Inhibition 5-lipoxygenase mediated LTB4 formation in rat basophilic leukemia (RBL-1) cells
- ChEMBL_1275645 (CHEMBL3090816) Inhibition of DOT1L (unknown origin)-mediated H3K79 methylation by cell based assay
- ChEMBL_1276667 (CHEMBL3089099) Inhibition of human IDO1-mediated tryptophan degradation expressed in human tumor cells
- ChEMBL_1346502 (CHEMBL3258076) Inhibition of SERT-mediated 5-HT uptake in Wistar rat brain synaptosomes
- ChEMBL_1436083 (CHEMBL3384714) Inhibition of BRAF (unknown origin)-mediated ERK phosphorylation by cell-based assay
- ChEMBL_2100811 (CHEMBL4809207) Inhibition of human OAT1 assessed as reduction in OAT1-mediated tenofovir transport
- ChEMBL_2100812 (CHEMBL4809208) Inhibition of human OAT3 assessed as reduction in OAT3-mediated tenofovir transport
- ChEMBL_2114003 (CHEMBL4822853) Inhibition of Escherichia coli GroEL/ES-mediated refolding of the denatured rhodanese
- ChEMBL_219634 (CHEMBL873393) Inhibition of human gel filtered platelet aggregation mediated by 10 uM ADP
- ChEMBL_28389 (CHEMBL875517) Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria
- ChEMBL_304163 (CHEMBL830001) GR-mediated transrepression of IL-6 in human A549 lung carcinoma cells
- ChEMBL_304193 (CHEMBL829188) Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
- ChEMBL_304224 (CHEMBL828940) Inhibition of GR-mediated tyrosine amino transferase activity in human HepG2 cells
- ChEMBL_305350 (CHEMBL832730) Concentration required for inhibition of HIV-1 integrase mediated 3'-end processing
- ChEMBL_306508 (CHEMBL828113) Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytes
- ChEMBL_310387 (CHEMBL834471) Inhibition of mu opioid receptor mediated GTPgammaS binding to CHO cell membranes
- ChEMBL_310403 (CHEMBL833181) Inhibition of delta opioid receptor mediated GTPgammaS binding to CHO cell membranes
- ChEMBL_310535 (CHEMBL834430) Effective concentration DP2 mediated expression of the adhesion molecule CD11b in eosinophils
- ChEMBL_322135 (CHEMBL885194) Effective concentration against US28-mediated inositol phosphate production in COS-7 cells
- ChEMBL_322381 (CHEMBL856245) Inhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulation
- ChEMBL_338364 (CHEMBL866544) Inhibition of D-glucose uptake mediated by PfHT expressed in Xenopus oocytes
- ChEMBL_353887 (CHEMBL865034) Inhibition of MCH-mediated calcium release in whole IMR32 cells by FLIPR
- ChEMBL_372238 (CHEMBL853391) Inhibition of SERT-mediated [3H]5-HT uptake in rat cerebral cortex
- ChEMBL_376178 (CHEMBL869315) Inhibition of mouse GAT1-mediated gamma-aminobutyric acid uptake in CHO cells
- ChEMBL_389612 (CHEMBL868623) Activity against AKT-mediated GSK3 S9P phosphorylation in human DOV13 cell line
- ChEMBL_389613 (CHEMBL868624) Activity against AKT-mediated PRAS40 T246P phosphorylation in human DOV13 cell line
- ChEMBL_40437 (CHEMBL652376) Inhibition of Bradykinin receptor B2-mediated contractions of rat uterus smooth muscle
- ChEMBL_430664 (CHEMBL919632) Inhibition of RFC-mediated [3H]MTX influx into human CCRF-CEM cells
- ChEMBL_458365 (CHEMBL941699) Inhibition of MMP13-mediated bovine nasal cartilage degradation assessed as hydroxyprole release
- ChEMBL_460516 (CHEMBL926596) Inhibition of human COX1-mediated conversion of arachidonic acid to prostaglandin-E2
- ChEMBL_462401 (CHEMBL927217) Inhibition of CXCR2-mediated chemotaxis in Ba/F3 cells expressing human CXCR2
- ChEMBL_462402 (CHEMBL927218) Inhibition of CXCR1-mediated chemotaxis in Ba/F3 cells expressing human CXCR1
- ChEMBL_465291 (CHEMBL933856) Inhibition of human integrin alpha5beta1 receptor mediated K562 cell adhesion to vitronectin
- ChEMBL_474153 (CHEMBL938411) Inhibition of Herpes B virus recombinant thymidine kinase-mediated [3H]TdR phosphorylation
- ChEMBL_489079 (CHEMBL987299) Inhibition of human recombinant p38alpha-mediated ATF2 phosphorylation by TR-FRET assay
- ChEMBL_492858 (CHEMBL942189) Inhibition of iNOS-mediated NO production in LPS-induced mouse BV2 cells
- ChEMBL_492926 (CHEMBL945314) Inhibition of SYK-mediated FCepsilonRI signaling activity by mast cell degranulation assay
- ChEMBL_494043 (CHEMBL938577) Inhibition of ABCB1-mediated [3H]vinblastine transportation in human Caco-2 cells
- ChEMBL_507896 (CHEMBL952593) Inhibition of human recombinant full length MMP13-mediated type 2 collagen cleavage
- ChEMBL_508956 (CHEMBL1005508) Inhibition of sheep COX2-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid
- ChEMBL_508957 (CHEMBL1005509) Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid
- ChEMBL_520160 (CHEMBL947848) Inhibition of human liver CE1-mediated O-nitrophenyl acetate hydrolysis by spectrophotometry
- ChEMBL_523245 (CHEMBL1000621) Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human WM266.4 cells
- ChEMBL_540456 (CHEMBL1029073) Inhibition of CDK4-mediated retinoblastoma protein phosphorylation by dose-response curve analysis
- ChEMBL_540457 (CHEMBL1029074) Inhibition of CDK2-mediated retinoblastoma protein phosphorylation by dose-response curve analysis
- ChEMBL_54504 (CHEMBL663852) Inhibitory concentration against human DNA topoisomerase II, alpha mediated relaxation of pBR322
- ChEMBL_552316 (CHEMBL1005220) Inhibition of Staphylococcus aureus MS5935 wild type DNA gyrase-mediated supercoiling activity
- ChEMBL_552317 (CHEMBL1005221) Inhibition of quinoline-resistant Staphylococcus aureus MS5935 DNA gyrase-mediated supercoiling activity
- ChEMBL_566626 (CHEMBL960940) Inhibition of c-Met-mediated scattering in HGF-stimulated human DU145 cells
- ChEMBL_577786 (CHEMBL1054713) Inhibition of FAAH-mediated hydrolysis of [3H]anandamide in rat RBL2H3 cells
- ChEMBL_579862 (CHEMBL1063248) Inhibition of human factor 10a-mediated cleavage of synthetic substrate S-2222
- ChEMBL_584629 (CHEMBL1059130) Inhibition of PLK1-mediated mitosis in human HeLaS3 cells after 18 hrs
- ChEMBL_597289 (CHEMBL1044320) Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human TF1 cells
- ChEMBL_597290 (CHEMBL1044321) Inhibition of JAK2-mediated STAT5 phosphorylation in GMCSF-stimulated human HT2 cells
- ChEMBL_60881 (CHEMBL673528) Compound was tested for the inhibition of E-selectin-mediated cellular adhesion
- ChEMBL_611773 (CHEMBL1066430) Mixed-type inhibition of autotaxin-mediated FS3 hydrolysis by Michaelis-Menten analysis
- ChEMBL_611775 (CHEMBL1066432) Competitive-type inhibition of autotaxin-mediated FS3 hydrolysis by Michaelis-Menten analysis
- ChEMBL_611779 (CHEMBL1066436) Noncompetitive inhibition of autotaxin-mediated pNP-TMP hydrolysis by Michaelis-Menten analysis
- ChEMBL_616144 (CHEMBL1103007) Inhibition of HSP90-mediated client protein HER2 degradation in human MCF7 cells
- ChEMBL_620469 (CHEMBL1099982) Competitive inhibition of PTP1B mediated pNPP hydrolysis by Lineweaver-Burke plot analysis
- ChEMBL_620931 (CHEMBL1117576) Inhibition of FAAH-mediated hydrolysis of [3H]AEA in rat brain membrane
- ChEMBL_631554 (CHEMBL1103919) Inhibition of c-Met-mediated scattering in HGF-stimulated human DU145 cells
- ChEMBL_633950 (CHEMBL1117631) Inhibition of VMAT2-mediated [3H]dopamine uptake in rat synaptic vesicle membranes
- ChEMBL_637676 (CHEMBL1166868) Inhibition of BACE1 mediated cleavage of amyloid precursor protein by chemiluminescence assay
- ChEMBL_638038 (CHEMBL1166941) Inhibition of IL5-mediated proliferation of mouse Y16 cells by WST1 assay
- ChEMBL_639647 (CHEMBL1175385) Inhibition of ABCG2-mediated drug efflux expressed in human NCI-H460 cells
- ChEMBL_646979 (CHEMBL1217120) Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human WM266.4 cells
- ChEMBL_654587 (CHEMBL1243631) Inhibition of human GST-fused Src-mediated Poly Glu4Tyr phosphorylation by ELISA
- ChEMBL_664340 (CHEMBL1259489) Inhibition of HIV-1 integrase-mediated 3'-processing and strand transfer activity
- ChEMBL_695894 (CHEMBL1640946) Inhibition of recombinant MPO mediated LDL oxidation using MPO/Cl-/H2O2 system
- ChEMBL_699336 (CHEMBL1647254) Inhibition of human recombinant CETP-mediated triglyceride transfer by fluorescence-based assay
- ChEMBL_741377 (CHEMBL1764903) Induction of human PPARdelta-mediated CPT1a gene expression in human skeletal muscle
- ChEMBL_741378 (CHEMBL1764904) Induction of human PPARdelta-mediated PDK4 gene expression in human skeletal muscle
- ChEMBL_770669 (CHEMBL1839794) Antagonist activity at integrin alpha2beta3-mediated aggregation in ADP-stimulated human platelets
- ChEMBL_788602 (CHEMBL1918637) Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in BHK cells
- ChEMBL_788603 (CHEMBL1918638) Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in BHK cells
- ChEMBL_788604 (CHEMBL1918639) Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in BHK cells
- ChEMBL_788605 (CHEMBL1918640) Inhibition of mouse GAT4-mediated [3H]GABA uptake expressed in BHK cells
- ChEMBL_797848 (CHEMBL1942434) Inhibition of mTOR-mediated p70S6K phosphorylation at Thr389 in human PC3 cells
- ChEMBL_802795 (CHEMBL1953529) Inhibition of human CCR2-mediated intracellular calcium mobilization by cell based assay
- ChEMBL_811063 (CHEMBL2014643) Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry
- ChEMBL_813833 (CHEMBL2020202) Inhibition of PI3Kalpha-mediated AKT phosphorylation at S473 by cell based assay
- ChEMBL_818324 (CHEMBL2034461) Inhibition of p38alpha-mediated TNFalpha secretion in LPS-stimulated human whole blood
- ChEMBL_823111 (CHEMBL2039633) Inhibition of MCP1-induced CCR2-mediated chemotaxis in human THP-1 cells
- ChEMBL_828305 (CHEMBL2050324) Inhibition of histamine H4 receptor-mediated chemotaxis in mouse bone marrow cells
- ChEMBL_831695 (CHEMBL2065058) Inhibition of mTOR-mediated AKT phosphorylation at Ser473 by cell based assay
- ChEMBL_835522 (CHEMBL2072228) Inhibition of Cdk5/p25-mediated myosin heavy chain phosphorylation in HEK293 cells
- ChEMBL_842390 (CHEMBL2092007) Inhibition of MEK1-mediated ERK1 phosphorylation after 30 mins by HTRF assay
- ChEMBL_856354 (CHEMBL2160709) Inhibition of telomerase-mediated primer elongation by gel electrophoresis-based TRAP assay
- ChEMBL_880259 (CHEMBL2215837) Inhibition of DAT-mediated [3H]DA in rat synaptomsomes by scintillation counting
- ChEMBL_880259 (CHEMBL2215837) Inhibition of DAT-mediated [3H]DA in rat synaptosomes by scintillation counting
- ChEMBL_887691 (CHEMBL2217300) Inhibition of PI3Kdelta-mediated AKT phosphorylation in human Ramos cells by ELISA
- ChEMBL_91794 (CHEMBL702301) Inhibition of LFA-1 mediated JY-8 cell adhesion to ICAM-1
- ChEMBL_938143 (CHEMBL2328225) Inhibition of PI3Kalpha-mediated AKT Ser 473 phosphorylation in human PC3 cells
- ChEMBL_940917 (CHEMBL2330563) Inhibition of ATM-mediated autophosphorylation at serine 1981 in human HT29 cells
- ChEMBL_945534 (CHEMBL2344011) Inhibition of human recombinant CYP2D6-mediated 7-methoxy-4(aminomethyl)-coumarine degradation
- ChEMBL_956924 (CHEMBL2378241) Inhibition of ovine COX2-mediated prostaglandin alpha production by enzyme immuno assay
- ChEMBL_956925 (CHEMBL2378242) Inhibition of ovine COX1-mediated prostaglandin alpha production by enzyme immuno assay
- ChEMBL_961183 (CHEMBL2389919) Inhibition of mPGES1-mediated PGE2 release in IL1alpha-stimulated human A549 cells
- ChEMBL_966070 (CHEMBL2395111) Inhibition of JAK1-mediated STAT3 phosphorylation in IL6-induced human TF1 cells
- ChEMBL_974258 (CHEMBL2411536) Inhibition of alpha4beta7 integrin-mediated human 8866 cell adhesion to MadCAM-1
- ChEMBL_977623 (CHEMBL2423590) Inhibition of SUMO E1 (unknown origin)-mediated RanGAP1 sumoylation by immunoblotting analysis
- ChEMBL_2362704 Inhibition of wild-type GDP-bound biotinylated-KRAS (unknown origin) assessed as suppression of SOS1-mediated nucleotide exchange by measuring reduction in KRAS-RAF RBD complex formation preincubated for 60 mins followed by SOS1 addition and further incubated for 60 mins and subsequent addition of KRAS-RAF RBD mixture measured after 30 to 60 mins by FRET assay
- ChEMBL_1555795 (CHEMBL3766570) Inhibition of mTOR kinase (unknown origin) assessed as suppression of ULight-4E-BP1 substrate phosphorylation incubated for 1 hr by lance ultra assay
- ChEMBL_1633674 (CHEMBL3876466) Activation of human S1PR4 expressed in CHO cells assessed as suppression of forskolin-induced intracellular cAMP level measured after 15 mins by ELISA
- ChEMBL_1772714 (CHEMBL4229706) Inhibition of C9 binding to C5b678 in zymogen activated human serum assessed as suppression of human erythrocyte lysis after 1 hr by ELISA
- ChEMBL_1777592 (CHEMBL4234584) Inhibition of human CaV3.1 expressed in HEK293 cells assessed as suppression of T-current after 10 mins by whole cell patch clamp method
- ChEMBL_2124454 (CHEMBL4833687) Inhibition of EZH2 Y641N mutant in human SU-DHL-6 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2124455 (CHEMBL4833688) Inhibition of EZH2 Y641S mutant in human SU-DHL-4 cells assessed as suppression H3K27 trimethylation measured after 72 hrs by immunoblot analysis
- ChEMBL_2291106 Antagonist activity at mouse CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary mouse T cells assessed as inhibition of CXCLI1 mediated cell migration incubated for 45 mins by Boyden chamber assay
- ChEMBL_2291107 Antagonist activity at human CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary human T cells assessed as inhibition of CXCLI1 mediated cell migration incubated for 45 mins by Boyden chamber assay
- ChEBML_1689719 Inhibition of PERK activation in rat INS-1 cells assessed as suppression of tunicamycin-induced CHOP mRNA expression after 8 hrs by qRT-PCR analysis
- ChEMBL_1498490 (CHEMBL3584608) Activation of GSK-3beta in HEK293 cells assessed as suppression of TCF/beta-catenin transcriptional activity after 24 hrs by SuperTOPFlash reporter gene assay
- ChEMBL_1544648 (CHEMBL3750621) Inhibition of PDE4 in human SHSY-5Y cells assessed as suppression of cAMP hydrolysis by HTRF assay in presence of dye d2 labelled cAMP
- ChEMBL_1755360 (CHEMBL4190120) Inhibition of ERK1/2 in human A375 cells harboring BRAF V600E mutant assessed as suppression of RSK phosphorylation after 4 hrs by MSD assay
- ChEMBL_1777587 (CHEMBL4234579) Inhibition of human CaV3.2 expressed in HEK293 cells assessed as suppression of T-current amplitude after 10 mins by whole cell patch clamp method
- ChEMBL_1809929 (CHEMBL4309389) Inhibition of IDH1/2 in human U87-MG cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
- ChEMBL_1905180 (CHEMBL4407538) Antagonist activity at human A1AR expressed in CHO cells assessed as suppression of CCPA-induced inhibition of forskolin-stimulated cAMP production by alphascreen assay
- ChEMBL_1911676 (CHEMBL4414122) Inhibition of of SHP2 in human KYSE520 cells assessed as suppression of ERK phosphorylation after 2 hrs by AlphaScreen SureFire Phospho-ERK1/2 assay
- ChEMBL_746464 (CHEMBL1776380) Inhibition of p38 alpha MAPK in human whole blood assessed as suppression of LPS-induced TNF-alpha release by immunosorbent non-radioactive enzyme assay
- ChEBML_208413 In vitro inhibition of Topoisomerase I-mediated DNA cleavage using supercoiled pBR322 plasmid DNA.
- ChEBML_208618 In vitro inhibition of Topoisomerase II-mediated DNA cleavage using supercoiled pBR322 plasmid DNA.
- ChEBML_214535 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEBML_214854 Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEBML_79564 Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA
- ChEBML_85066 In vitro antihistamine activity by activation of 4-methylhistamine mediated by Histamine H2 receptor
- ChEMBL_101112 (CHEMBL710208) Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferation
- ChEMBL_1351426 (CHEMBL3267002) Inhibition of mushroom tyrosinase-mediated L-tyrosine hydroxylation after 30 mins by ELISA
- ChEMBL_1354679 (CHEMBL3281104) Inhibition of human thrombin-mediated blood clotting formation in presence of human fibrinogen
- ChEMBL_1451472 (CHEMBL3364651) Inhibition of CETP-mediated [3H]-CE from HDL to LDL in human plasma
- ChEMBL_1492987 (CHEMBL3529116) Inhibition of recombinant CYP2J2 (unknown origin)-mediated terfenadine hydroxylation in presence of NADPH
- ChEMBL_1512557 (CHEMBL3610506) Inhibition of HSF1 (unknown origin) assessed as reduction in HSF1--mediated HSP transcription
- ChEMBL_157422 (CHEMBL768878) 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
- ChEMBL_1575613 (CHEMBL3803930) Inhibition of gamma secretase (unknown origin)-mediated notch processing by cell based assay
- ChEMBL_1622607 (CHEMBL3864959) Inhibition of 15-LOX-mediated lipid oxidation in 10% C57BL/6J mouse plasma
- ChEMBL_1772711 (CHEMBL4229703) Inhibition of human C2-mediated C3 processing after 24 hrs by SDS-PAGE
- ChEMBL_1902601 (CHEMBL4404823) Inhibition of JAK1/Tyk2-mediated STAT4 phosphorylation in IFNalpha-stimulated mouse whole blood
- ChEMBL_2022505 (CHEMBL4676318) Inhibition of Escherichia coli GroEL/ES-mediated refolding of the denatured malate dehydrogenase
- ChEMBL_2114002 (CHEMBL4822852) Inhibition of Escherichia coli GroEL/ES-mediated refolding of the denatured malate dehydrogenase
- ChEMBL_2114004 (CHEMBL4822854) Inhibition of human mitochondrial HSP60/10-mediated refolding of the denatured malate dehydrogenase
- ChEMBL_2126547 (CHEMBL4835892) Inhibition of human NTCP-mediated [3H]-TCA uptake expressed in human HepG2 cells
- ChEMBL_2155630 (CHEMBL5040290) Inhibition of SARS-COV2 spike protein mediated infection of human ACE2 expressing cells
- ChEMBL_221965 (CHEMBL842783) In vitro activity against topoisomerase-2 mediated cleavage of supercoiled pBR322 plasmid DNA
- ChEMBL_2227442 (CHEMBL5140955) Antagonist activity at human Androgen receptor measured by AR-mediated transcriptional activation assay
- ChEMBL_306509 (CHEMBL828114) Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes
- ChEMBL_310320 (CHEMBL833276) Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells
- ChEMBL_310464 (CHEMBL834409) Effective concentration towards human melanocortin-1 receptor mediated cAMP accumulation in CHO cells
- ChEMBL_310465 (CHEMBL825861) Effective concentration towards human melanocortin-3 receptor mediated cAMP accumulation in CHO cells
- ChEMBL_310466 (CHEMBL834410) Effective concentration towards human melanocortin-4 receptor mediated cAMP accumulation in CHO cells
- ChEMBL_310467 (CHEMBL834411) Effective concentration towards human melanocortin-5 receptor mediated cAMP accumulation in CHO cells
- ChEMBL_31877 (CHEMBL645667) Conversion of [32P] ATP to [32P]-cyclic AMP mediated by adenylate cyclase 1
- ChEMBL_322365 (CHEMBL884187) Inhibitory concentration against human glucagon-like peptide 1 receptor (hGLP1) mediated cAMP accumulation
- ChEMBL_365289 (CHEMBL862275) Induction of 5HT2C receptor mediated increase in intracellular calcium concentration in HEK293 cells
- ChEMBL_365290 (CHEMBL862276) Induction of 5HT2B receptor mediated increase in intracellular calcium concentration in CHO cells
- ChEMBL_365291 (CHEMBL862277) Induction of 5HT2A receptor mediated increase in intracellular calcium concentration in CHO cells
- ChEMBL_372182 (CHEMBL870441) Inhibition of human FATP4-mediated 12-BODIPY-lauric acid uptake in HEK293 cells
- ChEMBL_389619 (CHEMBL868630) Activity against AKT-mediated S6RP S235/236P phosphorylation in human DOV13 cell line
- ChEMBL_421987 (CHEMBL856549) Inhibition of MCH-mediated calcium release by CHO cells expressing human MCH-R1
- ChEMBL_424764 (CHEMBL907300) Inhibition of integrin alphavbeta3 mediated cell adhesion of human M21 cells to vitronectin
- ChEMBL_446267 (CHEMBL895371) Inhibition of human Pgp-mediated DNR transport in NIH3T3 cells by microplate assay
- ChEMBL_449874 (CHEMBL898978) Inhibition of integrin alpha-5-beta-1-mediated K562 cell adhesion to fibronectin
- ChEMBL_453271 (CHEMBL902426) Inhibition of gamma-secretase mediated amyloid beta-40 production in HEK293 cell membranes
- ChEMBL_455075 (CHEMBL887104) Inhibition of Kv1.5 channel mediated delayed rectifier potassium current by patch-clamp technique
- ChEMBL_460541 (CHEMBL927583) Inhibition of recombinant HIV1 integrase-mediated 3'-processing activity in presence of magnesium
- ChEMBL_460542 (CHEMBL927584) Inhibition of recombinant HIV1 integrase-mediated 3'-processing activity in presence of manganese
- ChEMBL_469905 (CHEMBL921229) Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells
- ChEMBL_476655 (CHEMBL927168) Inhibition of factor 5a-mediated prothrombin activation in human plasma by prothrombinase assay
- ChEMBL_483709 (CHEMBL954608) Inhibition of HIV1 protease-mediated proteolysis of rabbit muscle lactate dehydrogenase by spectrophotometry
- ChEMBL_490903 (CHEMBL989179) Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN negative human PC3 cells
- ChEMBL_490905 (CHEMBL989181) Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN negative human MCF7 cells
- ChEMBL_530431 (CHEMBL972196) Inhibition of FAAH mediated [14C]anandamide hydrolysis in rat brain after 30 mins
- ChEMBL_536732 (CHEMBL984526) Inhibition of 5-HT transporter-mediated [3H]5HT uptake in human Jar cells
- ChEMBL_549611 (CHEMBL1016757) Inhibition of LFA1/ICAM1-mediated adhesion of HL60 cells to CHO-ICAM1 cells
- ChEMBL_555234 (CHEMBL961375) Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells
- ChEMBL_594779 (CHEMBL1040740) Inhibition of mouse SGLT2-mediated [14C]alpha-methylglucopyranoside uptake by cell based assay
- ChEMBL_607731 (CHEMBL1066196) Inhibition of human PEPT1-mediated [3H]Gly-Sar uptake in human HeLa cells
- ChEMBL_611776 (CHEMBL1066433) Competitive-type inhibition of autotaxin-mediated pNP-TMP hydrolysis by Michaelis-Menten analysis
- ChEMBL_612179 (CHEMBL1073599) Inhibition of human glycine transporter 2-mediated glycine uptake expressed in HEK293 cells
- ChEMBL_619236 (CHEMBL1100403) Inhibition PI3K-alpha-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay
- ChEMBL_619469 (CHEMBL1107745) Inhibition PI3K-beta-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay
- ChEMBL_619470 (CHEMBL1107746) Inhibition PI3K-gamma-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay
- ChEMBL_619471 (CHEMBL1107747) Inhibition PI3K-delta-mediated PIP2 phosphorylation after 20 mins by alphascreen competition assay
- ChEMBL_625814 (CHEMBL1107112) Inhibition of gamma-secretase-mediated notch cleavage in human SNC cells by ELISA
- ChEMBL_634101 (CHEMBL1118885) Inhibition of gamma-secretase-mediated notch cleavage in human SNC cells by ELISA
- ChEMBL_660937 (CHEMBL1249604) Inhibition of Integrin alpha-4-beta-1-mediated adhesion in human jurkat cells
- ChEMBL_675741 (CHEMBL1272375) Inhibition of Pin1-mediated cyclin D1 expression in serum starved human PC3 cells
- ChEMBL_686949 (CHEMBL1291360) Inhibition of COX-2 mediated PGE2 production in LPS-induced mouse RAW264.7 cells
- ChEMBL_693079 (CHEMBL1638239) Inhibition of Mycobacterium smegmatis MC2 155 ATP synthase subunit c-mediated ATP production
- ChEMBL_699334 (CHEMBL1647252) Inhibition of human recombinant CETP-mediated cholesteryl ester transfer by fluorescence-based assay
- ChEMBL_699335 (CHEMBL1647253) Inhibition of CETP-mediated cholesteryl ester transfer in human serum after 1 hr
- ChEMBL_699551 (CHEMBL1647909) Induction of PPARdelta-mediated PDK4 mRNA upregulation in human myoblast after 24 hrs
- ChEMBL_730589 (CHEMBL1695310) Inhibition of human MDR1-mediated digoxin permeability expressed in pig LLC-PK1 cells
- ChEMBL_739729 (CHEMBL1763555) Inhibition of recombinant human VEGFR-2-mediated poly(Glu4Tyr) phosphorylation after 1 hr
- ChEMBL_745624 (CHEMBL1775994) Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_745625 (CHEMBL1775995) Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_745626 (CHEMBL1775996) Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_750666 (CHEMBL1785512) Inhibition of COX2-mediated PGE2 production in LPS-induced mouse MC3T3-E1 cells
- ChEMBL_773764 (CHEMBL1840130) Inhibition of JAK2-mediated STAT5 phosphorylation in human HEL 92.1.7 irf1-bla cells
- ChEMBL_786050 (CHEMBL1921660) Inhibition of PI3Kalpha-mediated Akt phosphorylation at Ser 473 in human U87MG cells
- ChEMBL_788301 (CHEMBL1919564) Inhibition of CYP2C9-mediated Tolbutamide methlyhydroxylation in human liver microsomes by LCMS analysis
- ChEMBL_788594 (CHEMBL1918629) Inhibition of mouse GAT1-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_788595 (CHEMBL1918630) Inhibition of mouse GAT2-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_788596 (CHEMBL1918631) Inhibition of mouse GAT3-mediated [3H]GABA uptake expressed in human HEK cells
- ChEMBL_794329 (CHEMBL1932251) Inhibition of human topoisomerase 1-mediated relation of supercoiled DNA after 45 mins
- ChEMBL_794336 (CHEMBL1932258) Inhibition of human topoisomerase 2-mediated relation of supercoiled DNA after 60 mins
- ChEMBL_799760 (CHEMBL1941466) Inhibition of RSK2-mediated CREB phosphorylation in HeLa cells expressing luciferase reporter gene
- ChEMBL_818207 (CHEMBL2034077) Inhibition of B-raf V600E mutant-mediated Erk phosphorylation in human Malme3 cells
- ChEMBL_827487 (CHEMBL2051344) Inhibition of xanthine oxidase- mediated uric acid formation after 5 mins by spectrophotometry
- ChEMBL_831696 (CHEMBL2065059) Inhibition of mTOR-mediated ribosomal protein S6 kinase phosphorylation by cell based assay
- ChEMBL_832969 (CHEMBL2066924) Inhibition of PAK4-mediated GEF-H1 phosphorylation at Ser810 by cell based assay
- ChEMBL_839705 (CHEMBL2089532) Inhibition to His6-tagged Sos1 catalytic domain-mediated nucleotide exchange by fluorimetric assay
- ChEMBL_840521 (CHEMBL2089872) Inhibition of Mps1-mediated p38 MAPK phosphorylation after 90 mins by DELFIA assay
- ChEMBL_861925 (CHEMBL2173729) Inhibition of human Carbonic anhydrase 9-mediated CO2 hydration by stopped-flow method
- ChEMBL_861926 (CHEMBL2173730) Inhibition of human Carbonic anhydrase 12-mediated CO2 hydration by stopped-flow method
- ChEMBL_861927 (CHEMBL2173731) Inhibition of human Carbonic anhydrase 2-mediated CO2 hydration by stopped-flow method
- ChEMBL_861928 (CHEMBL2173732) Inhibition of human Carbonic anhydrase 1-mediated CO2 hydration by stopped-flow method
- ChEMBL_86643 (CHEMBL693976) 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a
- ChEMBL_880263 (CHEMBL2215841) Inhibition of SERT-mediated [3H]5HT uptake in rat synaptosomes by scintillation counting
- ChEMBL_881929 (CHEMBL2212532) Inhibition of HIF-1alpha-mediated VEGF secretion in human Hep3b cells by ELISA
- ChEMBL_887687 (CHEMBL2217296) Inhibition of PI3Kdelta-mediated AKT phosphorylation in mouse Raw 264.7 cells by immunoassay
- ChEMBL_89710 (CHEMBL696413) Inhibition ADP-induced (fibrinogen-mediated) platelet aggregation in human platelet-rich plasma (PRP)
- ChEMBL_90320 (CHEMBL698534) Inhibition of human platelet aggregation mediated by alpha llb/beta3 interaction with fibrinogen
- ChEMBL_940916 (CHEMBL2330562) Inhibition of DNA-PK-mediated autophosphorylation at serine 2056 in human HT29 cells
- ChEMBL_940918 (CHEMBL2330564) Inhibition of PI3Kalpha-mediated AKT phosphorylation at threonine 308 in human BT474 cells
- ChEMBL_941898 (CHEMBL2329964) Inhibition of human recombinant IDE-mediated fluorescein-Abeta-(1-40)-Lys-biotin degradation
- ChEMBL_950696 (CHEMBL2352939) Inhibition of human recombinant MPO-mediated LDL oxidation after 5 mins by ELISA
- ChEMBL_975938 (CHEMBL2415587) Inhibition of mouse GAT3-mediated [3H]GABA uptake stably transfected in HEK293 cells
- ChEMBL_975939 (CHEMBL2415588) Inhibition of mouse GAT1-mediated [3H]GABA uptake stably transfected in HEK293 cells
- ChEMBL_975940 (CHEMBL2415589) Inhibition of mouse GAT2-mediated [3H]GABA uptake stably transfected in HEK293 cells
- ChEMBL_985785 (CHEMBL2434147) Inhibition of iNOS-mediated NO production in mouse RAW264.7 cells by Griess assay
- ChEBML_1619514 Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as suppression of 1'-hydroxymidazolam formation after 10 mins by LC-MS/MS analysis
- ChEMBL_1552424 (CHEMBL3761675) Inhibition of mPGES1 in LPS-induced human whole blood assessed as suppression of PGE2 response after 20 to 24 hrs by LC-MS/MS analysis
- ChEMBL_1809868 (CHEMBL4309328) Inhibition of IDH1 R132H mutant in human HT-1080 cells assessed as suppression of 2-HG production incubated for 48 hrs by LC-MS analysis
- ChEMBL_1932329 (CHEMBL4477981) Inhibition of SPT1 in human MCF7 cells assessed as suppression of 14C-serine incorporation into ceramide incubated for 2 hrs in presence of 4-HPR
- ChEMBL_2446497 Inhibition of XPO1 in human Jurkat cells assessed as suppression of IL-2 expression incubated for 6 hrs by Bright-Glo Luciferase based microplate reader analysis
- ChEBML_138301 In vitro contraction of guinea pig myenteric plexus preparation (mediated by muscarinic acetylcholine receptor M3)
- ChEBML_141047 In vitro concentration required to inhibit NHE-1 mediated intracellular maximal pH recovery by 50%
- ChEBML_48933 Inhibition of recombinant human CETP mediated transfer of [3H]cholesteryl ester from HDL to LDL
- ChEMBL_1279974 (CHEMBL3096609) Inhibition of rat Cav2.2-mediated calcium flux expressed in HEK cells by FDSS assay
- ChEMBL_1286430 (CHEMBL3112018) Inhibition of human recombinant carbonic anhydrase-2-mediated CO2 hydration by stopped-flow assay
- ChEMBL_1286431 (CHEMBL3112019) Inhibition of human recombinant carbonic anhydrase-1-mediated CO2 hydration by stopped-flow assay
- ChEMBL_138226 (CHEMBL744917) In vitro contraction of guinea pig myenteric plexus preparation (mediated by Muscarinic M3 receptor)
- ChEMBL_1458007 (CHEMBL3367181) Inhibition of AP-1-mediated collagenase production in IL1alpha-stimulated Lewis rat synovial cells
- ChEMBL_1492986 (CHEMBL3529115) Inhibition of recombinant CYP2J2 (unknown origin)-mediated astemizole O-demethylation in presence of NADPH
- ChEMBL_177560 (CHEMBL784318) Inhibitory activity against nAChR mediated nicotine-evoked [3H]DA overflow using rat striatal slices
- ChEMBL_2067903 (CHEMBL4723156) Inhibition of human TMPRSS2-mediated SARS-CoV-2 entry into human Caco-2 cells
- ChEMBL_212252 (CHEMBL876414) Inhibition of integrin alpha-v/beta-6 mediated UCLAP-3 cell adhesion to fibronectin
- ChEMBL_212254 (CHEMBL876415) Inhibition of integrin alpha-v/beta-5 mediated UCLAP-3 cell adhesion on vitronectin
- ChEMBL_214533 (CHEMBL819370) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214534 (CHEMBL819371) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214535 (CHEMBL819372) Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214851 (CHEMBL824693) Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_214854 (CHEMBL821469) Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_2158549 (CHEMBL5043299) Inhibition of CD69 (unknown origin) assessed as reduction in BCR mediated B cell activation
- ChEMBL_217362 (CHEMBL822875) Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated
- ChEMBL_2193358 (CHEMBL5105718) Inhibition of alphavbeta3 integrin receptor-mediated cell adhesion to fibrinogen in human HEK293 cells
- ChEMBL_221659 (CHEMBL823236) Inhibition of p60 c-Src tyrosine kinase mediated phosphorylation of Fak in IC8.1 fibroblasts
- ChEMBL_2272524 Antagonist activity against LasR-mediated quorum sensing system in Pseudomonas aeruginosa PAO1 by spectrophotometric assay
- ChEMBL_2276356 Inhibition of PCSK9 mediated LDLR degradation in human HepG2 cells assessed as restoration of LDLR
- ChEMBL_310334 (CHEMBL840822) Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 3 receptor
- ChEMBL_310335 (CHEMBL833290) Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 4 receptor
- ChEMBL_310336 (CHEMBL832470) Concentration of compound at 50% maximum cAMP accumulation mediated by human melanocortin 5 receptor
- ChEMBL_312139 (CHEMBL824877) Inhibition of 5-lipoxygenase mediated LTB4 synthesis in A-23187 simulated human whole blood
- ChEMBL_313640 (CHEMBL835784) Glucocorticoid receptor mediated transrepression of NFkB reporter gene in human A549 lung epithelial cells
- ChEMBL_322134 (CHEMBL885193) Effective concentration for cAMP accumulation mediated by human Melanocortin 4 receptor in HEK293 cells
- ChEMBL_329318 (CHEMBL863541) Activity against recombinant rat 5HT2C mediated intracellular calcium mobilization by FLIPR in SR3T3 cells
- ChEMBL_362619 (CHEMBL853229) Inhibition of GR-mediated transactivation of galactosidase reporter gene in HEK293 cells expressing 11betaHSD1
- ChEMBL_422114 (CHEMBL908799) Inhibition of Kv1.5 mediated ultra-rapid delayed rectifier current Ikur in human atrial cells
- ChEMBL_456206 (CHEMBL888216) Inhibition of AP1-mediated gene transcription in HepG2 cells by luciferase reporter gene assay
- ChEMBL_465975 (CHEMBL931159) Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells
- ChEMBL_465978 (CHEMBL931162) Inhibition of human BCRP pump mediated [3H]mitoxantrone transport in human Caco-2 cells
- ChEMBL_469850 (CHEMBL949038) Inhibition of MK2-mediated anisomycin-stimulated p38alpha phosphorylation in HeLa cells by flow cytometry
- ChEMBL_469914 (CHEMBL921238) Inhibition of inducible NOS mediated nitric oxide production in LPS-activated Kunming mouse macrophages
- ChEMBL_477688 (CHEMBL925844) Inhibition of human URAT1-mediated urate uptake in rat renal brush border membrane vesicles
- ChEMBL_477691 (CHEMBL925847) Inhibition of human URAT1-mediated urate uptake in HEK293 cells by competitive inhibition assay
- ChEMBL_48938 (CHEMBL661652) Inhibition of recombinant human CETP-mediated transfer of [3H]CE from HDL to LDL
- ChEMBL_490178 (CHEMBL983837) Inhibition of human recombinant His-tagged p38alpha-mediated ATF2 phosphorylation by TR-FRET assay
- ChEMBL_492346 (CHEMBL948342) Inhibition of recombinant TK1-mediated phosphorylation of [CH3-3H]deoxythymidine in presence of dithiothreitol
- ChEMBL_508178 (CHEMBL1008236) Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr
- ChEMBL_508179 (CHEMBL1008237) Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr
- ChEMBL_536861 (CHEMBL991671) Inhibition of MEK1-mediated ERK phosphorylation in human WM266-4 cells after 2.5 hrs
- ChEMBL_552857 (CHEMBL958062) Inhibition of 17-beta-HSD1-mediated 17-beta-estradiol formation in human T47D cells
- ChEMBL_553966 (CHEMBL965384) Inhibition of progesterone receptor mediated progesterone-induced alkaline phosphatase activity in human T47D cells
- ChEMBL_559466 (CHEMBL1018147) Inhibition of COX2-mediated PGE2 production in LPS-stimulated mouse RAW264.7 cells by ELISA
- ChEMBL_592913 (CHEMBL1048416) Inhibition of BACE1 mediated human Swedish amyloid precursor protein peptide hydrolysis by HTRF assay
- ChEMBL_608111 (CHEMBL1074800) Inhibition of gamma-secretase-mediated NotchdeltaE cleavage in human HeLa cells by luciferase assay
- ChEMBL_613843 (CHEMBL1067133) Inhibition of human recombinant AChE-mediated hydrolysis of acetylcholine by Lineweaver-Burke plot analysis
- ChEMBL_620496 (CHEMBL1107564) Inhibition of bovine milk XOR-mediated uric acid formation after 15 mins by spectrophotometer
- ChEMBL_627007 (CHEMBL1103663) Inhibition of human recombinant p38alpha-mediated AFT2 phosphorylation after 1 hr by HTRF assay
- ChEMBL_631553 (CHEMBL1103918) Inhibition of c-Met-mediated cell migration of human A549 cells by would healing
- ChEMBL_631855 (CHEMBL1111926) Inhibition of human DNA topoisomerase 1-mediated relaxation of supercoiled DNA by gel electrophoresis
- ChEMBL_631856 (CHEMBL1111927) Inhibition of human DNA topoisomerase 2-mediated relaxation of supercoiled DNA by gel electrophoresis
- ChEMBL_633352 (CHEMBL1120572) Inhibition of integrin alpha-V-beta-3-mediated adhesion of human cells M21 cells
- ChEMBL_654323 (CHEMBL1228671) Inhibition of BACE1-mediated cleavage of amyloid precursor protein after 16 hrs by spectrophotometry
- ChEMBL_676073 (CHEMBL1273067) Inhibition of bovine eNOS assessed as nitric oxide mediated oxidation of oxyhemoglobin to methemoglobin
- ChEMBL_694505 (CHEMBL1635795) Inhibition of sheep COX1-mediated PGE2 production after 2 mins by liquid scintillation counting
- ChEMBL_694506 (CHEMBL1635796) Inhibition of sheep COX2-mediated PGE2 production after 2 mins by liquid scintillation counting
- ChEMBL_697968 (CHEMBL1633028) Induction of ABCA1-mediated [3H]cholesterol efflux in mouse J774 macrophages after 4 hrs
- ChEMBL_700226 (CHEMBL1647327) Inhibition of gamma secretase-mediated amyloid beta42 production in HEK293 cells by sandwich immunoassay
- ChEMBL_727812 (CHEMBL1686295) Inhibition of integrin alpha4beta1-mediated Jurkat cell adhesion to VCAM-1 by FACS analysis
- ChEMBL_742336 (CHEMBL1768785) Inhibition of PDK1-mediated AKT phosphorylation at Ser473 in human PC3 cells by ELISA
- ChEMBL_743750 (CHEMBL1767564) Inhibition of wild type HIV-1 reverse transcriptase-mediated polymerization reaction after 30 mins
- ChEMBL_743751 (CHEMBL1767565) Inhibition of HIV-1 reverse transcriptase K101E mutant-mediated polymerization reaction after 30 mins
- ChEMBL_743752 (CHEMBL1767610) Inhibition of HIV-1 reverse transcriptase E138K mutant-mediated polymerization reaction after 30 mins
- ChEMBL_772090 (CHEMBL1837856) Inhibition of VEGFR2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_772096 (CHEMBL1837862) Inhibition of LYN-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_772152 (CHEMBL1838071) Inhibition of FGFR3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_772155 (CHEMBL1838074) Inhibition of FGFR1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773565 (CHEMBL1839931) Inhibition of FLT3-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773566 (CHEMBL1839932) Inhibition of TIE2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773567 (CHEMBL1839933) Inhibition of EPHB1-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773568 (CHEMBL1839934) Inhibition of PDGFRalpha-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773570 (CHEMBL1839936) Inhibition of MET-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773571 (CHEMBL1839937) Inhibition of SRC-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773598 (CHEMBL1839964) Inhibition of INSR-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773599 (CHEMBL1839965) Inhibition of JAK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773601 (CHEMBL1839967) Inhibition of RON-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773602 (CHEMBL1839968) Inhibition of ROS-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773604 (CHEMBL1839970) Inhibition of TYK2-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773605 (CHEMBL1839971) Inhibition of BMX-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_773606 (CHEMBL1839972) Inhibition of SYK-mediated proliferation of mouse BAF3 cells transformed with TEL-Kinase construct
- ChEMBL_786342 (CHEMBL1920538) Inhibition of human topoisomerase 2 alpha-mediated decatenation of kDNA by agarose gel electrophoresis
- ChEMBL_788299 (CHEMBL1919562) Inhibition of CYP2D6-mediated dextromethorphan O-demethylation in human liver microsomes by LCMS analysis
- ChEMBL_791578 (CHEMBL1930715) Inhibition of Human immunodeficiency virus 1 integrase-mediated strand transfer activity after 1 hr
- ChEMBL_79564 (CHEMBL686884) Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA
- ChEMBL_798335 (CHEMBL1943823) Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME-3M cells
- ChEMBL_799451 (CHEMBL1942259) Inhibition of PrCP-mediated conversion of Ang3 to Ang(2-7) in mouse plasma
- ChEMBL_804873 (CHEMBL1953791) Inhibition of human recombinant PDE4B2-mediated cAMP hydrolysis for 30 mins by colorimetric assay
- ChEMBL_807815 (CHEMBL1959593) Inhibition of PI3K p110alpha/p85alpha-mediated AKT1 phosphorylation at Ser473 in human U2OS cells
- ChEMBL_818502 (CHEMBL2032594) Antagonist activity at mouse MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
- ChEMBL_818575 (CHEMBL2032862) Antagonist activity at rat MCHR1 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
- ChEMBL_818577 (CHEMBL2032864) Antagonist activity at human MCHR2 assessed inhibition of MCH-mediated intracellular Ca2+ calcium mobilization
- ChEMBL_826174 (CHEMBL2049615) Inhibition of human BACE-1 mediated amyloid beta 40 release in human HEK293 cells
- ChEMBL_851654 (CHEMBL2157253) Inhibition of PI3Kdelta-mediated AKT phosphorylation in B cells in presence of human serum
- ChEMBL_854158 (CHEMBL2154079) Inhibition of COX2-mediated PGE2 production in LPS-induced mouse J774 cells by radioimmunoassay
- ChEMBL_861805 (CHEMBL2173398) Inhibition of SYK in peripheral blood monocytes assessed as reduction FcgammaR-mediated superoxide production
- ChEMBL_861806 (CHEMBL2173399) Inhibition of SYK in human U937 cells assessed as reduction FcgammaR-mediated superoxide production
- ChEMBL_873340 (CHEMBL2185193) Time dependent inhibition of CYP3A4-mediated testosterone-6-beta hydroxylation in human liver microsome
- ChEMBL_92286 (CHEMBL705832) Inhibition of AP-1 (activator protein-1) mediated transcriptional activation in Jurkat T-cells
- ChEMBL_939014 (CHEMBL2328716) Inhibition of mPGES1 mediated PGE2 production in LPS-stimulated human whole blood by ELISA
- ChEMBL_950697 (CHEMBL2352940) Inhibition of human recombinant MPO-mediated taurine chlorination after 5 mins by microplate assay
- ChEMBL_971564 (CHEMBL2406739) Induction of 5-HT4 receptor-mediated contraction in guinea pig longitudinal muscle myenteric plexus
- GR-Mediated Agonist Activity Assay and IL-6 Repression Assay GR-Mediated Agonist Activity Assay- GR-mediated activation by compounds is measured against maximal activation of dexamethasone in the same experiment and reported as % relative efficacy. Potencies of compounds are reported as the concentration at which they reach half their agonist (EC50). IL-6 Repression Assay- The GR-mediated repression of IL-6 production in a human fibroblast (NHDFneo) cell line is measured with a modified ELISA assay.
- ChEMBL_1619514 (CHEMBL3861683) Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate assessed as suppression of 1'-hydroxymidazolam formation after 10 mins by LC-MS/MS analysis
- ChEMBL_1624271 (CHEMBL3866683) Inhibition of FLAP in human monocytes assessed as suppression of fMLP/LPS-stimulated cys-LT formation preincubated for 15 mins measured after 10 mins by ELISA
- ChEMBL_1712876 (CHEMBL4122925) Inhibition of cIAP2 fused MALT1 (unknown origin) expressed in HEK293 cells assessed as suppression of NF-kB activation after 24 hrs by luciferase reporter gene assay
- ChEMBL_1878369 (CHEMBL4379763) Antagonist activity at human adenosine receptor A3 expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
- ChEMBL_1878370 (CHEMBL4379764) Antagonist activity at human adenosine receptor A2B expressed in CHO cells assessed as suppression of NECA-induced decrease of cAMP accumulation by Glo-sensor cAMP assay
- ChEMBL_1926331 (CHEMBL4429403) Inhibition of BTK in human peripheral B cells assessed as suppression of BCR/anti-IgM/IgG stimulated CD69 surface expression after 18 hrs by FACS analysis
- ChEMBL_863014 (CHEMBL2175194) Inhibition of STAT1 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT1-DNA interaction after 30 mins by EMSA
- ChEMBL_863016 (CHEMBL2175196) Inhibition of STAT3 dimerization in EGF-stimulated mouse NIH/3T3 cells overexpressing human EGFR assessed as suppression of STAT3-DNA interaction after 30 mins by EMSA
- ChEBML_139982 In vitro negative chronotropic effect on electrically driven guinea pig atria(mediated by Muscarinic M2 receptor)
- ChEBML_90526 Concentration required for inhibition of c-Src mediated phosphorylation of Fak in IC8.1 fibroblast cell assay
- ChEBML_91709 Increased outward current at -40 mV mediated by mouse KCNQ2 channel expressed in Xenopus laevis oocytes
- ChEMBL_1339915 (CHEMBL3243752) Inhibition of human recombinant MMP13-mediated amyloid beta hydrolysis after 10 mins by fluorimetry assay
- ChEMBL_1464308 (CHEMBL3404575) Inhibition of mouse IL5-mediated mouse Y16 cell proliferation after 48 hrs by WST1 assay
- ChEMBL_1467097 (CHEMBL3411294) Inhibition of human OATP1B3-mediated [3H]CCK-8 after 5 mins by Dixon plot method
- ChEMBL_1467136 (CHEMBL3411333) Inhibition of Mps1 (unknown origin)-mediated p38 MAPK phosphorylation after 90 mins by DELFIA assay
- ChEMBL_1487744 (CHEMBL3533738) Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake
- ChEMBL_1559661 (CHEMBL3779075) Inhibition of CDK8-mediated STAT1 phosphorylation at serine727 in human SW620 cells harboring APC mutant
- ChEMBL_1772705 (CHEMBL4229697) Inhibition of MASP-2-mediated C4 deposition in human serum after 1 hr by ELISA
- ChEMBL_1772706 (CHEMBL4229698) Inhibition of MASP-1-mediated C3 deposition in human serum after 30 mins by ELISA
- ChEMBL_1870467 (CHEMBL4371634) Antagonist activity at ETA receptor (unknown origin) assessed as increase in G protein-mediated vasoconstriction
- ChEMBL_2046416 (CHEMBL4701115) Inhibition of BTK in human Ramos cells assessed as reduction in BCR mediated PLCgamma2 phosphorylation
- ChEMBL_2198286 (CHEMBL5110802) Inhibition of DNA topoisomerase 2 alpha (unknown origin) measured by topoisomerase-mediated DNA relaxation assay
- ChEMBL_304255 (CHEMBL829726) GR-mediated transrepression of IL-6 in peritoneal exudate cells harvested from C57BI/6 mice
- ChEMBL_339267 (CHEMBL867222) Inhibition of TLR2 agonist Pam3Cys-Ser-(Lys)4-OH-mediated IL8 secretion in THP1 cells
- ChEMBL_425214 (CHEMBL855160) Antagonistic activity at rat bradykinin B1 receptor assessed as effect on DAK-mediated calcium mobilization
- ChEMBL_454874 (CHEMBL886904) Antagonist activity at MCHR1 assessed as inhibition of MCH-mediated calcium release in IMR32 cells
- ChEMBL_465290 (CHEMBL933855) Inhibition of human integrin alpha-V-beta-3 receptor mediated K562 cell adhesion to vitronectin
- ChEMBL_465292 (CHEMBL933857) Inhibition of human integrin alpha-v-beta-3 receptor mediated WM115 cell adhesion to vitronectin
- ChEMBL_465293 (CHEMBL933858) Inhibition of human integrin alpha-5-beta-1 receptor mediated WM115 cell adhesion to vitronectin
- ChEMBL_48933 (CHEMBL665928) Inhibition of recombinant human CETP mediated transfer of [3H]cholesteryl ester from HDL to LDL
- ChEMBL_508732 (CHEMBL1004026) Inhibition of HIV1 RT mediated DNA-dependent DNA synthesis initiation using DNA PPT-primed substrate
- ChEMBL_514847 (CHEMBL971751) Inhibition of B-Raf-mediated phosphorylation of MEK1 in mouse 3T3 cells after 2 hrs
- ChEMBL_532343 (CHEMBL973266) Induction of BK channel mediated vasorelaxation activity in Kcl-induced contraction in Wistar rat aorta
- ChEMBL_54505 (CHEMBL663853) Inhibitory concentration against human DNA topoisomerase II, alpha mediated relaxation of pBR322; no measurable activity
- ChEMBL_547549 (CHEMBL1033407) Inhibition of iNOS-mediated NO production in LPS-stimulated mouse RAW264.7 cells by Griess method
- ChEMBL_559467 (CHEMBL1018148) Inhibition of iNOS-mediated NO production in LPS-stimulated mouse RAW264.7 cells by Griess method
- ChEMBL_626134 (CHEMBL1116097) Inhibition of gamma-secretase-mediated Notch deltaE cleavage in human HeLa cells by luciferase assay
- ChEMBL_643089 (CHEMBL1176555) Inhibition of AKT1-mediated GSK3alpha phosphorylation in human U87 cells after 1 hr by ELISA
- ChEMBL_676071 (CHEMBL1273065) Inhibition of mouse macrophage iNOS assessed as nitric oxide mediated oxidation of oxyhemoglobin to methemoglobin
- ChEMBL_676072 (CHEMBL1273066) Inhibition of rat brain nNOS assessed as nitric oxide mediated oxidation of oxyhemoglobin to methemoglobin
- ChEMBL_753235 (CHEMBL1799390) Inhibition of human recombinant PRMT1-mediated arginine methylation using nonhistone protein Npl3 substrate by ELISA
- ChEMBL_757844 (CHEMBL1809788) Inhibition of human recombinant cytosolic carbonic anhydrase 1-mediated CO2 hydration activity after 15 mins
- ChEMBL_757845 (CHEMBL1809789) Inhibition of human recombinant cytosolic carbonic anhydrase 2-mediated CO2 hydration activity after 15 mins
- ChEMBL_757846 (CHEMBL1809790) Inhibition of human recombinant transmembrane carbonic anhydrase 9-mediated CO2 hydration activity after 15 mins
- ChEMBL_757847 (CHEMBL1809791) Inhibition of human recombinant transmembrane carbonic anhydrase 12-mediated CO2 hydration activity after 15 mins
- ChEMBL_795811 (CHEMBL1936698) Inhibition of human RSK2-mediated CREB phosphorylation in HLR-CREB cells by cell based assay
- ChEMBL_802466 (CHEMBL1955040) Inhibition of B-Raf V600E mutant-mediated ERK phosphorylation in human WM266.4 cells by ELISA
- ChEMBL_807805 (CHEMBL1959583) Inhibition of BACE-1-mediated sAPPbeta production in human SH-SY5Y cells after 16 hrs
- ChEMBL_956334 (CHEMBL2379568) Inhibition of MAGL-mediated 2-arachidonoylglycerol hydrolysis in mouse brain membranes preincubated for 30 mins