BDBM50103608 Anti-Lewisite Sulfactin Dimercaprol CHEBI:64198
BDBM50332839 anti(2S,5'S)-(+)-5b3-Methyl-5-pyrrolidin-2-yl-4,5-dihydroisoxazole CHEMBL1630288
BDBM50332901 anti-(3S)-4-(4-(benzyloxy)phenyl)-2-hydroxy-3-palmitamidobutylphosphonic acid CHEMBL1632524 CHEMBL1632523
CHEMBL1630293 BDBM50332835 anti(2S,5'S)-(+)-3-Methoxy-5-pyrrolidin-2-yl-4,5-dihydroisoxazole
CHEMBL1766010 BDBM50342134 Methyl anti-3-(1H-1-Imidazolyl)-3-[4-(phenylamino)phenyl]-2-methylpropanoate
BDBM50332917 anti-(3S)-4-(4-(2,4-dichlorobenzyloxy)phenyl)-2-hydroxy-3-palmitamidobutylphosphonic acid CHEMBL1632615 CHEMBL1632614
CHEMBL1630295 anti(2S,5'S)-(+)-3-tert-butoxy-5-pyrrolidin-2-yl-4,5-dihydroisoxazole BDBM50332837
CHEMBL1632618 CHEMBL1632617 BDBM50332921 anti-(3S)-4-(4-(3,5-dimethylbenzyloxy)phenyl)-2-hydroxy-3-palmitamidobutylphosphonic acid
CHEMBL1766012 BDBM50342136 Methyl anti-3-(1H-1-Imidazolyl)-3-[4-(2-naphthylamino)phenyl]-2-methylpropanoate
anti-(3S)-4-(4-(2,4-dimethylbenzyloxy)phenyl)-2-hydroxy-3-palmitamidobutylphosphonic acid BDBM50332915 CHEMBL1632613 CHEMBL1632612
(1R,2S,5S,6S)-3-azabicyclo[3.1.0]hexane-2,6-dicarboxylic acid Anti-endo-MPDC CHEMBL1256243 BDBM50327886
CHEMBL1259100 anti-2-Amino-5-oxo-4,7-diphenyl-4,5,7,8-tetrahydropyrano[4,3-b]-pyran-3-carbonitril BDBM50328521
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- ChEMBL_2102732 (CHEMBL4811128) Inhibition of PD1/PD-L1 (unknown origin)
- ChEMBL_2016504 (CHEMBL4670082) Inhibition of PD1-Tag2/PD-L1-Tag1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 measured after 3 hrs by HTRF assay
- ChEMBL_2023624 (CHEMBL4677437) Inhibition of PD1-Tag2/PD-L1-Tag1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 measured after 2.5 hrs by HTRF assay
- ChEMBL_2232295 (CHEMBL5146067) Inhibition of Tag2-PD1/Tag1-PD-L1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 and measured after 2 hrs by HTRF analysis
- ChEMBL_2083844 (CHEMBL4739635) Antagonist activity at PD1/PD-L1 (unknown origin)
- ChEMBL_2119759 (CHEMBL4828906) Inhibition of Tag2-PD1/Tag1-PD-L1 (unknown origin) protein-protein interaction preincubated for 15 mins followed by addition of anti-Tag1-Eu3+ and anti-Tag2-XL665 measured after 2 hrs in dark by HTRF assay
- ChEMBL_2016502 (CHEMBL4670080) Binding affinity to PD1 (unknown origin) by SPR analysis
- ChEMBL_2083843 (CHEMBL4739634) Antagonist activity at human PD1/PD-L1 preincubated with PD-L1 for 1 hr followed by incubation with PD1 for 1 hr by ELISA
- ChEMBL_1988151 (CHEMBL4621698) Inhibition of human C-terminal Ig-Fc-tagged PD1 (Leu25 to Gln167 residues) expressed in HEK293 cells/human C-terminal epitope-His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction preincubated for 15 mins with PDL1 followed by PD1 addition and measured after 15 mins by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
- ChEMBL_1830219 (CHEMBL4330227) Inhibition of PD1/PDL1 (unknown origin) interaction by HTRF assay
- ChEMBL_1980087 (CHEMBL4613349) Inhibition of human PD1/PDL1 protein-protein interaction by HTRF assay
- ChEMBL_1988149 (CHEMBL4621696) Inhibition of human PD1/PDL1 protein-protein interaction by HTRF assay
- ChEMBL_1497759 (CHEMBL3583018) Binding affinity to His-tagged PD-L1 (unknown origin) assessed as inhibition of interaction with PD1 preincubated for 15 mins followed by PD1 addition measured after 15 mins by HTRF assay
- ChEMBL_1830221 (CHEMBL4330229) Inhibition of PD1/PDL1 interaction (unknown origin) after 15 mins by HTRF assay
- ChEMBL_2094006 (CHEMBL4775269) Binding affinity to PDL1 (unknown origin) assessed as reduction in PDL1/PD1 protein-protein interaction preincubated for 15 mins followed by PD1 addition and measured after 15 mins by HTRF binding assay
- ChEMBL_1813372 (CHEMBL4312946) Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 1 hr by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
- ChEMBL_1988150 (CHEMBL4621697) Inhibition of human Fc-tagged PD1 N-terminal domain (Leu25 to Gln167 residues) expressed in HEK293 cells/human His-tagged PDL1 (Phe19 to Arg238 residues) expressed in HEK293 cells protein-protein interaction after 40 mins by APC-labeled anti-His antibody/Eu-labeled anti-human IgG based HTRF assay
- ChEMBL_1892502 (CHEMBL4394423) Inhibition of human PD1/PDL1 protein-protein interaction after 15 mins by HTRF assay
- ChEMBL_1991569 (CHEMBL4625304) Inhibition of PD1 (unknown origin)/PDL1 (unknown origin) protein-protein interaction by HTRF assay
- ChEMBL_2110970 (CHEMBL4819820) Inhibition of PD1 (unknown origin)/PDL1 (unknown origin) protein-protein interaction by HTRF assay
- ChEMBL_2119765 (CHEMBL4828912) Inhibition of PD1/PDL1 protein-protein interaction in human Jurkat cells overexpressing PD1 co-cultured with human Hep3B cells expressing PDL1 protein assessed as increase of TCR-mediated luminiscence measured after 6 hrs by NFAT reporter assay
- ChEMBL_2079473 (CHEMBL4735264) Inhibition of PD1/PDL1 (unknown origin) protein-protein interaction measured after 15 mins by HTRF assay
- ChEMBL_1667595 (CHEMBL4017391) Binding affinity to His-tagged PD-L1 (unknown origin) assessed as reduction in PD-L1/PD1-Ig interaction preincubated with PD-L1 for 15 mins followed by addition of PD1-Ig measured after 15 mins by HTRF assay
- ChEMBL_2034715 (CHEMBL4688873) Antagonist activity at human PDL1 assessed as inhibition of human PD1 interaction with human PDL1 by ELISA
- ChEMBL_2101027 (CHEMBL4809423) Inhibition of PD1/PD-L1 (unknown origin) protein-protein interaction measured after 135 mins by HTRF assay
- ChEMBL_2132501 (CHEMBL4842016) Inhibition of human PD1/PDL1 protein-protein interaction expressed in Escherichia coli BL21 (DE3) by HTRF assay
- ChEMBL_1849390 (CHEMBL4349931) Transrepression of RORgammat in Balb/c mouse splenocytes assessed as reduction in anti-CD3/anti-CD28 stimulated IL-17 level measured after 48 hrs in presence of anti-CD3/anti-CD28 by ELISA
- ChEMBL_1931330 (CHEMBL4434581) Inhibition of Ig-tagged human PD1/His-tagged human PDL1 interaction incubated for 30 mins by HTRF assay
- ChEMBL_2127474 (CHEMBL4836819) Inhibition of human PD1/PDL1 protein-protein interaction assessed as undissociated complex after 2 hrs by HTRF assay
- ChEMBL_1666750 (CHEMBL4016546) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-CD3/anti-CD28-mediated IFNgamma production preincubated for 1 hr followed by anti-CD3/anti-CD28 activation measured after overnight incubation by AlphaLisa assay
- anti-cytopathic effect in a Vero-E6 cell line anti-cytopathic effect in a Vero-E6 cell line.
- ChEBML_208331 Anti- Thrombin activity using standard chromogenic assay
- ChEMBL_214568 (CHEMBL856235) Anti-vasopressor activity at V1a receptor
- ChEMBL_214569 (CHEMBL818694) Anti-vasopressor activity at V1a receptor
- ChEMBL_2102731 (CHEMBL4811127) Inhibition of PD1/PD-L1 (unknown origin) protein-protein interaction measured after 135 mins by TR-FRET assay relative to control
- ChEMBL_1830210 (CHEMBL4330218) Binding affinity to human PD1 (34 to 150 residues) expressed in Escherichia coli BL21 (DE3) measured for 120 secs by SPR analysis
- ChEMBL_1830215 (CHEMBL4330223) Inhibition of PD1/PDL1 interaction in human jurkat cells co-expressing TCR promoter assessed as TCR activation by luciferase reporter gene assay
- ChEMBL_1830220 (CHEMBL4330228) Inhibition of recombinant human PD1 (25 to 167 residues)/human PDL1 (19 to 238 residues) interaction after 40 mins by HTRF assay
- ChEMBL_2017407 (CHEMBL4670985) Binding affinity to human PD1-L1 (18-134 residues) expressed in Escherichia coli BL21 (DE3) incubated for 1 hr by MST analysis
- ChEMBL_225580 (CHEMBL847936) In vitro anti-thrombin activity was determined
- ChEMBL_2035337 (CHEMBL4689495) Inhibition of HPK1 in anti-CD3/anti-CD28-stimulated human T-cells assessed as inhibition of SLP76 phosphorylation preincubated for 1 hr followed by anti-CD3/CD28 stimulation for 30 mins by AlphaLISA assay
- ChEMBL_2016501 (CHEMBL4670079) Inhibition of FC-tagged PD1/His-tagged PD-L1 (unknown origin) protein-proteiinteraction incubated for 3 hrs by coimmunoprecipitation-based Western blot assay
- ChEMBL_618643 (CHEMBL1101692) Inhibition of deoxycytidine kinase in anti CD3 and anti CD28 -stimulated mouse T cells assessed as reduction in [3H]deoxycitidine incorporation
- ChEMBL_618644 (CHEMBL1101693) Inhibition of deoxycytidine kinase in anti CD3 and anti CD28 -stimulated human T cells assessed as reduction in [3H]deoxycitidine incorporation
- ChEBML_151696 Compound was evaluated for anti-platelet activating factor potency
- ChEBML_35865 Antithrombin III (ATIII)-mediated anti-Xa activity was determined
- ChEMBL_149198 (CHEMBL762760) In vitro anti-oxytocic activity with out Mg2+.
- ChEMBL_211859 (CHEMBL819243) Compound was evaluated for its anti tubulin activity
- ChEMBL_149197 (CHEMBL762759) In vitro anti-oxytocic activity with 0.5 mM Mg2+.
- ChEMBL_149201 (CHEMBL762763) In vitro anti-oxytocic activity with 0.5 mM Mg2+.
- ChEMBL_211356 (CHEMBL815872) The compound was evaluated for the anti-tubulin activity.
- ChEMBL_878239 (CHEMBL2185027) Covalent inhibition of ITK in human whole blood assessed as inhibition of anti-CD3 antibody-stimulated IL2 production pre-incubated before anti-CD3 antibody challenge
- ChEBML_207781 Anti-synthetase activity against TXA2 synthase in human whole blood assay
- ChEMBL_2321742 Inhibition of PI3Kdelta in anti-FceRI-stimulated human Basophil cells degranulation
- ChEMBL_2424480 Inhibition of PLCgamma2 phosphorylation in anti-IgM activated human Ramos cells
- ChEMBL_2060119 (CHEMBL4715120) Inverse agonist activity at RORgammat in human whole blood assessed as inhibition of anti-CD3/anti-CD28 monoclonal antibodies-stimulated IL-17A production measured by ELISA
- ChEMBL_1852030 (CHEMBL4352654) Inhibition of PI3Kgamma in human whole blood assessed as reduction in anti-IgE-stimulated CD63 expression in basophils preincubated for 30 mins followed by anti-IgE stimulation
- ChEMBL_2014995 (CHEMBL4668573) Inhibition of CFD in human RBC model of anti-CD55/anti-CD59-induced paroxysmal nocturnal hemoglobinuria assessed as reduction in complement fragment C3 deposition by FACS analysis
- ChEMBL_1988186 (CHEMBL4621733) Inhibition of mouse biotin-labelled C-terminal Fc-fused/Avi-tagged PD1/Fc-fused PDL1 expressed in HEK293 cells protein-protein interaction measured after 2 hrs by ELISA
- ChEMBL_149193 (CHEMBL762756) In vitro activity for the anti-oxytocic activity with out Mg2+
- ChEMBL_149194 (CHEMBL762757) In vitro activity for the anti-oxytocic activity with out Mg2+.
- ChEMBL_149199 (CHEMBL762761) In vitro activity for the anti-oxytocic activity with out Mg2+.
- ChEMBL_214570 (CHEMBL818695) Compound was evaluated for the anti-vasopressor activity at V1a receptor..
- ChEMBL_304773 (CHEMBL828539) Anti-oxidant activity in DPPH radical scavenging assay; n=3-4
- ChEMBL_311665 (CHEMBL825457) Anti-oxidant activity in DPPH radicak scavenging assay; n=3-4
- ChEMBL_350443 (CHEMBL861681) Inhibition of anti-CD3 antibody-induced IL2 production in human PBMC
- ChEMBL_87880 (CHEMBL698799) In vitro for anti-HD2 (Histone deacetylase 2) activity in maize
- ChEMBL_1926302 (CHEMBL4429374) Inhibition of BTK in human RamosB cells assessed as suppression of BCR/anti-IgM stimulated calcium flux pre-incubated for 1 hr followed by BCR/anti-IgM stimulation
- ChEMBL_2318351 Inhibition of human HPK1 in anti-humanCD3/anti-humanCD28 stimulated human CD3-positive T cells assessed as increase in IL-2 release incubated for 48 hrs by AlphaLISA assay
- ChEMBL_599136 (CHEMBL1047191) Inhibition of PKCtheta in C57BL/6 mouse T cells assessed as inhibition of anti-CD3 and anti-CD28-induced IL2 production after 20 to 24 hrs by ELISA
- ChEMBL_878242 (CHEMBL2185030) Covalent inhibition of ITK in human Jurkat cells assessed as inhibition of anti-CD3 antibody-stimulated PLCgamma phosphorylation pre-incubated before anti-CD3 antibody challenge by Western blotting
- ChEMBL_2083840 (CHEMBL4739631) Antagonist activity at PD1/PD-L1 (unknown origin) assessed as disruption of PD-1/PD-L1 complex by measuring PD-L1 dimerization measured after 2 hrs by HTRF assay
- ChEMBL_1766681 (CHEMBL4201928) Inhibition of anti-IgM-stimulated BTK phosphorylation at Tyr551 in human Ramos cells pre-incubated for 1 hr followed by anti-IgM stimulation for 10 mins by Western blotting
- ChEMBL_1766682 (CHEMBL4201929) Inhibition of anti-IgM-stimulated BTK phosphorylation at Tyr223 in human Ramos cells pre-incubated for 1 hr followed by anti-IgM stimulation for 10 mins by Western blotting
- 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
- ChEMBL_1987160 (CHEMBL4620707) Inverse agonist activity at RORgammat in human whole blood assessed as inhibition of anti-CD3/anti-CD28 monoclonal antibodies-stimulated IL-17A production measured after 3 days by ELISA
- ChEMBL_1830666 (CHEMBL4330674) Anti-biofilm activity against Enterococcus faecalis after 24 hrs by XTT assay
- ChEMBL_90699 (CHEMBL702100) In vitro anti-HIV integrase activity against 3' processing of target plasmid.
- Cell Based Assay To assess phosphor-EGFR signaling, blots were probed with rabbit anti-Phospho-EGFR (Y1068) and mouse total anti-EGFR antibodies. Phospho-EGFR signal was normalized to total EGFR expression for each sample. To assess phosphor-S6 ribosomal protein signaling, blots were probed with mouse anti-phosphor-S6 ribosomal protein and rabbit total anti-S6 ribosomal protein. Blots were normalized as indicated above. Results are indicated as % DMSO control.
- ChEMBL_1766683 (CHEMBL4201930) Inhibition of anti-IgM-stimulated BTK-mediated PLCgamma2 phosphorylation at Tyr1217 in human Ramos cells pre-incubated for 1 hr followed by anti-IgM stimulation for 10 mins by Western blotting
- ChEMBL_2019502 (CHEMBL4673080) Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in anti-IgM-induced AKT phosphorylation at Ser473 residue preincubated for 20 mins followed by anti-IgM stimulation for 30 mins
- ChEBML_29230 Inhibitory concentration in vitro and ex vivo for anti-AChE activity in rat brain
- ChEMBL_328617 (CHEMBL863865) Inhibitory activity against anti-CD3 mAb-induced IL2 production in human whole blood
- ChEMBL_350436 (CHEMBL861673) Inhibition of anti-CD3 antibody-induced IL2 production in human jurkat T cells
- ChEMBL_87865 (CHEMBL697288) In vitro for anti-HDAC1 (Histone deacetylase 1) activity in mouse A20 cells
- ChEMBL_90700 (CHEMBL702101) In vitro anti-HIV integrase activity against integration (strand transfer) of target plasmid.
- ChEMBL_1473873 (CHEMBL3418950) Inhibition of Syk in anti-CD32 stimulated CD14+ human monocytes assessed as phospho-SLP76 level preincubated for 30 mins followed by anti-CD32 stimulation measured after 5 mins by flow cytometric analysis
- PD-1/PD-L1 Homogeneous Time-Resolved Fluorescence (HTRF) Binding Assay The assays were conducted in a standard black 384-well polystyrene plate with a final volume of 20 μL. Inhibitors were first serially diluted in DMSO and then added to the plate wells before the addition of other reaction components. The final concentration of DMSO in the assay was 1%. The assays were carried out at 25° C. in the PBS buffer (pH 7.4) with 0.05% Tween-20 and 0.1% BSA. Recombinant human PD-L1 protein (19-238) with a His-tag at the C-terminus was purchased from AcroBiosystems (PD1-H5229). Recombinant human PD-1 protein (25-167) with Fc tag at the C-terminus was also purchased from AcroBiosystems (PD1-H5257). PD-L1 and PD-1 proteins were diluted in the assay buffer and 10 pt was added to the plate well. Plates were centrifuged and proteins were preincubated with inhibitors for 40 minutes. The incubation was followed by the addition of 10 μL of HTRF detection buffer supplemented with Europium cryptate-labeled anti-human IgG (PerkinElmer-AD0212) specific for Fc and anti-His antibody conjugated to SureLight -Allophycocyanin (APC, PerkinElmer-AD0059H). After centrifugation, the plate was incubated at 25° C. for 60 min. before reading on a PHERAstar FS plate reader (665 nm/620 nm ratio). Final concentrations in the assay were −3 nM PD1, 10 nM PD-L1, 1 nM europium anti-human IgG and 20 nM anti-His-Allophycocyanin.
- ChEMBL_1473872 (CHEMBL3418949) Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis
- ChEMBL_1473914 (CHEMBL3419165) Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-CD3 stimulation measured after 2 mins by FACS analysis
- ChEMBL_1521567 (CHEMBL3627445) Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis
- ChEMBL_1719215 (CHEMBL4134215) Inhibition of PI3Kdelta in Balb/c mouse splenocytes assessed as reduction in anti-IgM stimulated CD86 expression pretreated for 1 hr followed by anti-IgM stimulation after 24 hrs by flow cytometric analysis
- ChEMBL_1926977 (CHEMBL4430049) Inhibition of PI3Kdelta in Balb/c mouse B cells assessed as reduction in anti-IgM induced CD86 expression preincubated for 1 hr followed by anti-IgM stimulation for 24 hrs by flow cytometry
- ChEMBL_1926983 (CHEMBL4430055) Inhibition of PI3Kdelta in human B cells assessed as reduction in anti-human IgM stimulated CD86 expression preincubated for 1 hr followed by anti-human IgM stimulation for 24 hrs by flow cytometry
- ChEMBL_1926984 (CHEMBL4430056) Inhibition of PI3Kdelta in human B cells assessed as reduction in anti-human IgM stimulated CD69 expression preincubated for 1 hr followed by anti-human IgM stimulation for 24 hrs by flow cytometry
- ChEMBL_1929866 (CHEMBL4433042) Inhibition of SYK in human Ramos cells assessed as suppression of anti-IgM induced Erk1/2 phosphorylation preincubated for 30 mins followed by anti-IgM addition measured after 7 mins by electrochemiluminescence analysis
- ChEMBL_1970419 (CHEMBL4603237) Inhibition of PI3K delta in human whole blood assessed as inhibition of anti-IgE-stimulated CysLt release in basophils preincubated for 30 mins followed by anti-IgE stimulation and measured after 20 mins
- ChEMBL_2019503 (CHEMBL4673081) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-CD79b antibody-induced CD69 expression preincubated for 60 mins followed by anti-CD79b antibody stimulation for 3 hrs by FACS analysis
- ChEMBL_2051225 (CHEMBL4705924) Inhibition of MALT1 in human whole blood assessed as reduction in PMA//anti-CD28 antibody-induced IL2 level pre-incubated for 1 hrs before stimulation with PMA//anti-CD28 antibody by MSD assay
- ChEMBL_2110234 (CHEMBL4818909) Inhibition of BTK in C57Bl/6 mouse splenocyte assessed as reduction in anti-IgM-induced CD69 expression incubated for 1 hr followed anti-IgM stimulation and measured after overnight by flow cytometry analysis
- ChEMBL_2236549 (CHEMBL5150445) Inhibition of BTK autophosphorylation in anti-IgG stimulated human DOHH-2 cells preincubated for 1 hr followed by compound washout and anti-IgG stimulation for 2 mins by chemiluminescence based Western blotting analysis
- ChEMBL_149195 (CHEMBL882485) In vitro activity was determined for the anti-oxytocic activity with 0.5 mM Mg2+.
- ChEMBL_149200 (CHEMBL762762) In vitro activity was determined for the anti-oxytocic activity with 0.5 mM Mg2+.
- ChEMBL_155797 (CHEMBL760283) In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase C59R/S108N (K1CB1) mutant
- ChEMBL_155800 (CHEMBL765485) In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase N51I/C59R/S108N (W2)
- ChEMBL_155801 (CHEMBL765486) In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase wild type (TM4/8.2)
- ChEMBL_1673721 (CHEMBL4023750) Inhibition of anti-IgM-induced BTK phosphorylation at Y233 in human primary B cells
- ChEMBL_1706715 (CHEMBL4057948) Inhibition of BTK in human PBMC assessed as reduction in anti-IgM-induced MIP1beta
- ChEMBL_2024271 (CHEMBL4678084) Inhibition of IRAK4 in human THP-1 cells by cell based anti-inflammatory assay
- ChEMBL_1337883 (CHEMBL3240910) Inhibition of SYK in human whole blood assessed as anti-human IgM-induced CD69 protein expression preincubated for 30 mins followed by anti-human IgM addition measured after 20 hrs by flow cytometric analysis
- ChEMBL_1845467 (CHEMBL4345894) Inhibition of RORgammat in human whole blood assessed as reduction in anti-CD3/anti-CD28 monoclonal antibodies/IL-18/IL-23-stimulated IL-17A production incubated for 2 days by mesoscale assay kit method
- ChEMBL_1929869 (CHEMBL4433045) Inhibition of SYK in human B cells assessed as suppression of anti-IgM-induced CD69 surface expression preincubated for 30 mins followed by anti-IgM addition measured after 3.5 hrs by flow cytometric analysis
- ChEMBL_1971004 (CHEMBL4603822) Inhibition of ITK in anti-CD3/CD28 beads-stimulated human Jurkat cells assessed as reduction in Plcgamma1 phosphorylation incubated for 2 hrs followed by stimulation with anti-CD3/CD28 beads by Western blot analysis
- ChEMBL_2157143 (CHEMBL5041803) Inhibition of HPK1 in human Jurkat E6.1 cells assessed as SLP76 phosphorylation incubated for 30 mins followed by anti-CD3, biotinylated anti-SLP76 and TMB substrate addition measured after 3 hrs by ELISA assay
- PDL1/PD1 Binding Assay Compounds to be tested were serially diluted in DMSO, and further diluted in assay buffer (25 mM Hepes pH 7.4, 150 mM NaCl, 0.005% Tween 20, BSA 0.01%). Diluted compounds were added to the wells with final concentration of DMSO at 1%. PDL1-6×His protein was added to the wells, mixed well with compound. The plates were incubated for 30 min at room temperature. PD1-Fc-Avi-Biotin protein was added to the wells. Final concentration of PDL1 and PD1 protein is 0.3 nM and 2.5 nM, respectively. After a binding time of 30 min at room temperature, Anti-6×His Acceptor beads (final concentration 20 ug/ml) were added to the wells, and the incubation continued for 1 h. Streptavidin Donor beads (final concentration 20 ug/mL) were added at reduced light. The plates were sealed with foil and incubated in the dark for additional 1 h or overnight before reading on an Envision reader.
- ChEMBL_1651105 (CHEMBL4000360) Inhibition of BTK in human Ramos cells assessed as inhibition of anti human IgM-induced calcium influx preincubated for 20 mins in dark followed by anti human IgM induction for 8 mins by FLIPR assay
- ChEMBL_1719218 (CHEMBL4134218) Inhibition of PI3Kdelta in human B cells assessed as reduction in anti-IgM-induced AKT phosphorylation at ser473 residue pretreated for 1.5 hrs followed by anti-IgM stimulation after 20 mins by flow cytometric analysis
- ChEMBL_1719219 (CHEMBL4134219) Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD86 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis
- ChEMBL_1719220 (CHEMBL4134220) Inhibition of PI3Kdelta in 90% human whole blood assessed as reduction in anti-IgM/IL4 stimulated CD69 expression pretreated for 1 hr followed by anti-IgM/IL4 stimulation after 24 hrs by flow cytometric analysis
- ChEMBL_1848293 (CHEMBL4348834) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-CD79b antibody-induced CD69 expression preincubated for 60 mins followed by anti-CD79b antibody stimulation and measured after 3 hrs by FACS analysis
- ChEMBL_1977991 (CHEMBL4611126) Inhibition of PKCbeta in rat RBL2H3 cells assessed as inhibition of anti-DNP IgE-stimulated TNFalpha release preincubated for 15 mins followed by mouse anti-DNP IgE stimulation and measured after 3 hrs by ELISA
- ChEMBL_1977995 (CHEMBL4611130) Inhibition of PKC in rat RBL2H3 cells assessed as inhibition of anti-DNP IgE-stimulated TNFalpha release preincubated for 15 mins followed by mouse anti-DNP IgE stimulation and measured after 3 hrs by ELISA
- ChEMBL_2126109 (CHEMBL4835454) Inhibition of PI3Kdelta in human whole blood assessed as reduction in anti-CD79b antibody-induced CD69 expression preincubated for 60 mins followed by anti-CD79b antibody stimulation and measured after 3 hrs by FACS analysis
- Homogeneous Time-Resolved Fluorescence (HTRF) PD1/PD-L1 binding assay kit (Cisbio, Cat #63ADK000CPDEC) was used, which includes two proteins, Tag 1-PD-L1 and Tag 2-PD-1, and two antibodies, Anti-Tag1-Eu3+ and Anti-Tag2-XL 665. Assay principle: Anti-tag1-Eu3+ is the HTRF donor, and Anti-Tag2-XL 665 is the HTRF acceptor. When Tag 1-PD-L1 and Tag 2-PD-1 interact, the added HTRF donor and the acceptor are close to each other. After the donor receives the excitation energy, it transfers part of the energy to the acceptor, thus producing 665 nm emission signal. When the compound is added to block the PD1/PD-L1 interaction, only 620 nm emission light was detected. The inhibitory effect of the compound was determined by analyzing the ratio of 665 nm/620 nm. Tag 1-PD-L1 was diluted with Diluent buffer (cat #62DLBDDF) to a working concentration of 10 nM, Tag 2-PD-1 was diluted with Diluent buffer to a working concentration of 500 nM, and Anti-Tag1-Eu3+ was diluted with detection buffer (cat #62DB1FDG) by 1:100, Anti-Tag2-XL 665 was diluted with detection buffer by 1:20, and the test compound was diluted with Diluent buffer to a final concentration of 2×. In a 384-well plate, 2 μL of compound was added to each well, and then 4 μL of Tag 1-PD-L1, 4 μL of Tag 2-PD-1 were added and incubated at room temperature for 15 minutes.
- Homogeneous Time-Resolved Fluorescence (HTRF) PD-1/PD-L1 Binding Assay The assays were conducted in a standard black 384-well polystyrene plate with a final volume of 20 μL. Inhibitors were first serially diluted in DMSO and then added to the plate wells before the addition of other reaction components. The final concentration of DMSO in the assay was 1%. The assays were carried out at 25° C. in the PBS buffer (pH 7.4) with 0.05% Tween-20 and 0.1% BSA. Recombinant human PD-L1 protein (19-238) with a His-tag at the C-terminus was purchased from AcroBiosystems (PD1-H5229). Recombinant human PD-1 protein (25-167) with Fc tag at the C-terminus was also purchased from AcroBiosystems (PD1-H5257). PD-L1 and PD-1 proteins were diluted in the assay buffer and 10 μL was added to the plate well. Plates were centrifuged and proteins were preincubated with inhibitors for 40 minutes. The incubation was followed by the addition of 10 μL of HTRF detection buffer supplemented with Europium cryptate-labeled anti-human IgG (PerkinElmer-AD0212) specific for Fc and anti-His antibody conjugated to SureLight -Allophycocyanin (APC, PerkinElmer-AD0059H). After centrifugation, the plate was incubated at 25° C. for 60 min. before reading on a PHERAstar FS plate reader (665 nm/620 nm ratio). Final concentrations in the assay were 3 nM PD1, 10 nM PD-L1, 1 nM europium anti-human IgG and 20 nM anti-His-Allophycocyanin.
- PD-1/PD-L1 Homogeneous Time-Resolved Fluorescence (HTRF) Binding Assay Assays were performed in standard black 384-well polystyrene plates and a final volume was 20 L. The inhibitor was first serially diluted with DMSO and added to the wells of the plate, then other reaction components were added. The final concentration of DMSO in the assay was 1%. Assays were performed at 25 C. in PBS buffer (pH 7.4) containing 0.05% Tween-20 and 0.1% BSA. Recombinant human PD-L1 protein (19-238) with a His-tagged at the C-terminus was purchased from AcroBiosystems (PD1-H5229). Recombinant human PD-1 protein (25-167) with an Fc tag at the C-terminus was also purchased from AcroBiosystems (PD1-H5257). The PD-L1 and PD-1 proteins were diluted in assay buffer and then 0.1 l of the solution was extracted and added to the wells of the plate. Plates were centrifuged and proteins and inhibitors were preincubated for 40 minutes. After incubation, 0.1 l of HTRF detection buffer containing europium blocking labeled anti-human IgG (PerkinElmer-AD0212), Fc-specific and anti-His SureLight -Allophycocyanin (APC, PerkinElmer-AD0059H) conjugated antibodies was added. After centrifugation, the plates were incubated at 25 C. for 60 minutes. Data was read in a PHERAstar FS plate reader (665 nm/620 nm ratio). Final concentrations in the assay were ~3 nM of PD1, 10 nM of PD-L1, 1 nM of europium anti-human IgG, and 20 nM of anti-His-allophycocyanin.
- PD-1/PD-L1 Homogeneous Time-Resolved Fluorescence (HTRF) Binding Assay The assays were conducted in a standard black 384-well polystyrene plate with a final volume of 20 μL. Inhibitors were first serially diluted in DMSO and then added to the plate wells before the addition of other reaction components. The final concentration of DMSO in the assay was 1%. The assays were carried out at 25° C. in the PBS buffer (pH 7.4) with 0.05% Tween-20 and 0.1% BSA. Recombinant human PD-L1 protein (19-238) with a His-tag at the C-terminus was purchased from AcroBiosystems (PD1-H5229). Recombinant human PD-1 protein (25-167) with Fc tag at the C-terminus was also purchased from AcroBiosystems (PD1-H5257). PD-L1 and PD-1 proteins were diluted in the assay buffer and 10 μL was added to the plate well. Plates were centrifuged and proteins were preincubated with inhibitors for 40 minutes. The incubation was followed by the addition of 10 μL of HTRF detection buffer supplemented with Europium cryptate-labeled anti-human IgG (PerkinElmer-AD0212) specific for Fc and anti-His antibody conjugated to SureLight -Allophycocyanin (APC, PerkinElmer-AD0059H). After centrifugation, the plate was incubated at 25° C. for 60 min. before reading on a PHERAstar FS plate reader (665 nm/620 nm ratio). Final concentrations in the assay were −3 nM PD1, 10 nM PD-L1, 1 nM europium anti-human IgG and 20 nM anti-His-Allophycocyanin.