PACAP-38 PACAP PACAP38 CHEMBL524658 BDBM50250019 PACAP(1-38)
PACAP(5-27) PACAP(6-27) BDBM81529
PACAP(6-27) PACAP(7-27) BDBM81530
[Phe1]PACAP(1-27) [Phe1]PACAP-27 BDBM82399
BDBM50250068 PACAP-27 [Glu3]PACAP27 CHEMBL501240 PACAP(1-27)
[DPhe2]PACAP(1-27) BDBM81526 [D-Phe2]PACAP-27
[DPhe2]PACAP(1-38) BDBM81531 [D-Phe2]PACAP-38
PACAP-VIP BDBM82358
VIP-PACAP BDBM82362
BDBM81528 PACAP(7-38)
BDBM81534 PACAP(4-38)
BDBM81761 PACAP(4-27)
BDBM81765 PACAP(9-38)
BDBM81821 PACAP(3-25)
BDBM81826 PACAP(1-23)
BDBM82356 PACAP(2-38)
BDBM82361 PACAP(2-27)
BDBM82440 PACAP(6-31)
BDBM82442 PACAP(6-35)
BDBM82449 PACAP(11-27)
PACAP(10-38) BDBM82444
PACAP(11-38) BDBM82453
PACAP(3-27) BDBM81532
PACAP(3-38) BDBM81763
PACAP(5-27) BDBM81527
PACAP(5-38) BDBM81536
PACAP(8-27) BDBM81764
PACAP(8-38) BDBM81762
PACAP(9-27) BDBM82445
BDBM81524 [Phe2]PACAP(1-38)
BDBM81535 CHEMBL525267 PACAP(6-38)
BDBM81540 [Asn3]PACAP(1-27)
BDBM81824 PACAP(1-33,Cys34)
BDBM82447 [DAla2]PACAP(1-38)
BDBM82448 [Ala2]PACAP(1-27)
BDBM82450 [AcHis1]PACAP(1-27)
BDBM82451 [DArg2]PACAP(1-27)
[Arg2]PACAP(1-27) BDBM82443
[Arg2]PACAP(1-38) BDBM82452
[DAla2]PACAP(1-27) BDBM82441
[DArg2]PACAP(1-38) BDBM82446
[Phe2]PACAP(1-27) BDBM81533
BDBM81525 [AcHis1,Phe2]PACAP(1-38)
BDBM81537 [AcHis1,DPhe2]PACAP(1-27)
BDBM81538 [AcHis1,Phe2]PACAP(1-27)
BDBM81539 [AcHis1,DPhe2]PACAP(1-38)
BDBM81760 [Des-His1,Glu3]PACAP-38
[Des-His1,Asn3]PACAP-27 BDBM81759
BDBM81825 PACAP(1-23),VIP(24-28)
2,3-dihydroxybenzohydroxamoyl adenylate BDBM50186354
BDBM27683 [adenylate-32P]-NAD
BDBM50250023 [Ala2]PACAP38 CHEMBL500280 [Ala2]PACAP(1-38)
CHEMBL526552 BDBM50250064 [Asn3]PACAP(1-27) [Asn3]PACAP27
Aminoalkyl adenylate and aminoacyl sulfamate analogue BDBM50091515
CAS_37221-79-7 Vasoactive intestinal polypeptide VIP(4-28) BDBM81828
ATP-gammaS ATPgammaS ADENOSINE-5'-DIPHOSPHATE MONOTHIOPHOSPHATE BDBM50118217 CHEMBL131890 PHOSPHOTHIOPHOSPHORIC ACID-ADENYLATE ESTER
(3S)-3-amino-4-[({[(2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy}(hydroxy)phosphoryl)oxy]butanoic acid BDBM18124 L-aspartol adenylate, 5
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- Takahashi, H; Riether, D; Bartolozzi, A; Bosanac, T; Berger, V; Binetti, R; Broadwater, J; Chen, Z; Crux, R; De Lombaert, S; Dave, R; Dines, JA; Fadra-Khan, T; Flegg, A; Garrigou, M; Hao, MH; Huber, J; Hutzler, JM; Kerr, S; Kotey, A; Liu, W; Lo, HY; Loke, PL; Mahaney, PE; Morwick, TM; Napier, S; Olague, A; Pack, E; Padyana, AK; Thomson, DS; Tye, H; Wu, L; Zindell, RM; Abeywardane, A; Simpson, T Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915). J Med Chem 58: 1669-90 (2015)
- ChEMBL_31725 (CHEMBL646264) Effective concentration against adenylate cyclase
- ChEBML_31727 Effective concentration required to stimulate Adenylate cyclase
- ChEBML_31418 In vitro inhibition of dopamine stimulated adenylate cyclase
- ChEMBL_220725 (CHEMBL844231) Antagonist potency in hCRF1 stimulated adenylate cyclase assay
- ChEMBL_31721 (CHEMBL646260) Compound was tested for the adenylate cyclase stimulation
- ChEMBL_31571 (CHEMBL644534) Inhibitory concentration against Dopamine sensitive adenylate cyclase in rats
- ChEMBL_31583 (CHEMBL646377) Inhibitory activity against Dopamine sensitive adenylate cyclase in rats
- ChEMBL_85065 (CHEMBL692776) Inhibitory activity against brain adenylate cyclase Histamine H2 receptor
- ChEBML_217935 KB for inhibition of adenylate cyclase stimulation in human platelet membranes
- ChEBML_31715 Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
- ChEBML_31885 Inhibition of recombinant human adenylate cyclase 5 expressed in HEK293 cells
- ChEMBL_31292 (CHEMBL643973) In vitro inhibitory activity against glucagon induced monkey adenylate cyclase
- ChEMBL_31423 (CHEMBL645297) In vitro inhibitory activity against glucagon induced human adenylate cyclase
- ChEMBL_31425 (CHEMBL645299) In vitro inhibitory activity against glucagon induced human adenylate cyclase
- ChEMBL_60359 (CHEMBL672094) Potency in adenylate cyclase functional assay against Dopamine receptor D1
- ChEBML_214869 Inhibition of LVP-sensitive adenylate cyclase in a pig renal medullary preparation
- ChEBML_31442 Inhibition of LVP stimulated adenylate cyclase activity in pig kidney medullary membrane
- ChEMBL_1973 (CHEMBL617578) Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor
- ChEMBL_27761 (CHEMBL643366) Potency against human platelet A2 adenosine receptor by adenylate cyclase activation
- ChEMBL_27945 (CHEMBL649126) Potency against PC12 cell A2 adenosine receptor by adenylate cyclase activation
- ChEMBL_31713 (CHEMBL645373) Effective concentration as Adenylate cyclase activity was measured in rat homogenate
- ChEMBL_31714 (CHEMBL645374) Compound was evaluated for inhibition of adenylate cyclase from rat brain
- ChEMBL_31715 (CHEMBL645375) Inhibitory concentration against rat striatal dopamine (D1) sensitive adenylate cyclase activity
- ChEMBL_810 (CHEMBL767044) Inhibition of forskolin stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor
- ChEBML_31291 Displacement of [125I]6-IHPP-Fsk from adenylate cyclase of bovine brain membrane
- ChEBML_31582 Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart
- ChEMBL_27763 (CHEMBL643368) Stimulation of adenylate cyclase activity in human platelet membrane at A2 receptor
- ChEMBL_28544 (CHEMBL640323) Inhibition of adenylate cyclase via A1 receptors in rat fat cell membranes
- ChEMBL_31572 (CHEMBL644535) The compound was tested for adenylate cyclase activity in rat corpus striatum
- ChEMBL_31878 (CHEMBL645668) Inhibition of [125 I]6-IHPP-forskolin binding to adenylate cyclase 1
- ChEMBL_31879 (CHEMBL645669) Inhibition of [125 I]6-IHPP-forskolin binding to adenylate cyclase 1
- ChEMBL_31880 (CHEMBL645670) Inhibition of [125 I]6-IHPP-forskolin binding to Adenylate cyclase 1
- ChEMBL_31884 (CHEMBL645674) Inhibitory activity against recombinant human adenylate cyclase 5 expressed in HEK293 cells.
- ChEMBL_27610 (CHEMBL875808) Maximal NECA stimulation of adenylate cyclase via A2 receptors in human platelet membranes
- ChEMBL_28545 (CHEMBL640324) Inhibition of adenylate cyclase via Adenosine A1 receptor in rat fat cell membranes
- ChEMBL_28546 (CHEMBL640325) Inhibition of adenylate cyclase via adenosine A1 receptors in rat fat cell membranes
- ChEMBL_29627 (CHEMBL636645) Inhibition of adenylate cyclase via Adenosine A1 receptor in rat fat cell membranes
- ChEMBL_30603 (CHEMBL642010) Inhibition of NECA-induced stimulation of adenylate cyclase at human adenosine A2B receptor
- ChEMBL_31569 (CHEMBL645175) Tested for ability to stimulate dopamine sensitive adenylate cyclase in rat caudate homogenate
- ChEMBL_31582 (CHEMBL646376) Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart
- ChEMBL_31729 (CHEMBL646267) Tested for effective dose agonist activity against adenylate cyclase in rat striatal membrane
- ChEMBL_31877 (CHEMBL645667) Conversion of [32P] ATP to [32P]-cyclic AMP mediated by adenylate cyclase 1
- ChEMBL_215035 (CHEMBL820885) Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
- ChEMBL_217362 (CHEMBL822875) Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated
- ChEMBL_27612 (CHEMBL644331) Maximal NECA stimulation of adenylate cyclase via Adenosine A2 receptor in human platelet membranes
- ChEMBL_27762 (CHEMBL643367) Maximal NECA stimulation of adenylate cyclase via adenosine A2 receptor in human platelet membranes
- ChEMBL_28543 (CHEMBL640322) Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor
- ChEMBL_28671 (CHEMBL644726) Maximal NECA stimulation of adenylate cyclase via Adenosine A2 receptor in human platelet membranes
- ChEMBL_30867 (CHEMBL873059) Maximal NECA stimulation of adenylate cyclase via Adenosine A2 receptor in human platelet membranes.
- ChEMBL_31438 (CHEMBL645311) Compound was evaluated for inhibition of hormone stimulated Adenylate cyclase activity in N18TG2 membranes.
- ChEMBL_59895 (CHEMBL673021) Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2
- ChEMBL_60358 (CHEMBL672093) Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1
- ChEMBL_830343 (CHEMBL2060977) Agonist activity at D1 receptor in rat striatum assessed as synaptosomal adenylate cyclase activity
- ChEBML_1768 Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
- ChEBML_1972 Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1D receptor of rat substantia nigra
- ChEBML_214852 Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
- ChEBML_214867 Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
- ChEBML_593 Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
- ChEBML_604 Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
- ChEMBL_153751 (CHEMBL761206) Tested for inhibition of rat PC12 adenylate cyclase stimulation by using NECA as a radioligand
- ChEMBL_217361 (CHEMBL822874) Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
- ChEMBL_220717 (CHEMBL843662) Activity of peptidic agonists on h-CRF2-alpha receptor using agonist-stimulated adenylate cyclase assay
- ChEMBL_30854 (CHEMBL643571) Tested for inhibition of rat PC12 adenylate cyclase stimulation by using NECA as a radioligand
- ChEMBL_89563 (CHEMBL697366) Inhibition of 5'-(N-ethylcarbamoyl)adenosine-elicited stimulation of adenylate cyclase in human platelet membranes
- ChEMBL_951348 (CHEMBL2354035) Antagonist activity at A3 adenosine receptor (unknown origin) assessed as inhibition of adenylate cyclase activity
- ChEBML_1668 Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1D receptor of guinea pig substantia nigra
- ChEMBL_1767 (CHEMBL616552) Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
- ChEMBL_1768 (CHEMBL832876) Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
- ChEMBL_214852 (CHEMBL824694) Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
- ChEMBL_214867 (CHEMBL820053) Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
- ChEMBL_27927 (CHEMBL642335) Inhibition of NECA binding to adenosine A2 receptor mediates reduced adenylate cyclase activity in human platelets
- ChEMBL_290 (CHEMBL615728) Effect on forskolin stimulated adenylate cyclase activity at 5-HT1D receptor of guinea pig substantia nigra.
- ChEMBL_50954 (CHEMBL666036) Effective concentration to stimulate the human corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
- ChEMBL_58663 (CHEMBL670437) Dopamine receptor D1 antagonistic activity as ability to block dopamine-stimulated adenylate cyclase in rat caudate
- ChEMBL_593 (CHEMBL615463) Effect on forskolin stimulated adenylate cyclase activity at 5-hydroxytryptamine 1A receptor of guinea pig hippocampus.
- ChEMBL_60198 (CHEMBL673360) Ability to inhibit the dopamine-stimulated adenylate-cyclase activity in dispersed cells of bovine parathyroid gland
- ChEMBL_604 (CHEMBL615473) Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
- ChEMBL_869 (CHEMBL615924) Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
- ChEMBL_870 (CHEMBL615925) Inhibition of forskolin-activated adenylate cyclase (cAMP) activity at 5-hydroxytryptamine 1A receptor in rat hippocampus
- ChEMBL_139108 (CHEMBL749232) Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M4
- ChEMBL_139619 (CHEMBL744784) Reversal of forskolin-stimulated accumulation of adenylate cyclase in transfected CHO cells, against Muscarinic acetylcholine receptor M2
- ChEMBL_1672 (CHEMBL616663) Ability to inhibit forskolin-stimulated adenylate cyclase in a cell line expressing human 5-hydroxytryptamine 1D receptor
- ChEMBL_211247 (CHEMBL878965) Ability to inhibit AVP stimulation of adenylate cyclase activity in the rat kidney medulla (AVP-V2) receptor
- ChEMBL_27756 (CHEMBL641992) Inhibition of 2-CADO-stimulated adenylate cyclase at Adenosine A2 receptor in guinea pig cerebral cortical slices
- ChEMBL_27784 (CHEMBL645920) Binding affinity for adenosine A2 receptor using [3H]- NECA antagonism of adenylate cyclase activation in human platelets
- ChEMBL_31296 (CHEMBL643977) Binding activity against Adenylate cyclase in bovine brain membrane using [125I]6-IHPP-Fsk as the radioligand.
- ChEMBL_31876 (CHEMBL645666) Ability to activate the conversion of [32P] ATP to [32P]-cyclic AMP mediated by adenylate cyclase 1
- ChEMBL_478884 (CHEMBL937355) Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase
- ChEMBL_60523 (CHEMBL674934) Dopamine D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes
- ChEMBL_746178 (CHEMBL1775792) Agonist activity at human GPR119 expressed in human HEK293 cells assessed as increase in adenylate cyclase activation
- ChEBML_214692 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in dog
- ChEBML_214849 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEBML_591 Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1A receptor in guinea pig
- ChEMBL_27918 (CHEMBL642326) In vitro binding affinity to Adenosine A2 receptor of human platelets by inhibition of NECA-stimulated adenylate cyclase
- ChEMBL_878512 (CHEMBL2188177) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as NECA-induced adenylate cyclase activity
- ChEMBL_214849 (CHEMBL824691) In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEMBL_214850 (CHEMBL824692) In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEMBL_31026 (CHEMBL638315) Antagonism of N-ethylcarboxamido adenosine-stimulated adenylate cyclase associated with stimulation of Adenosine A2 receptor of rat PC12 membranes
- ChEMBL_31424 (CHEMBL645298) In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
- ChEMBL_603083 (CHEMBL1038805) Agonist activity at human 5HT1A receptor expressed in CHO cells assessed as inhibition of forskolin-induced adenylate cyclase activity
- ChEBML_1651 Compound was tested for the inhibition of forskolin-stimulated adenylate cyclase at 5-hydroxytryptamine 1D receptor in guinea pig substantia nigra
- ChEMBL_2075 (CHEMBL875905) In vitro effective concentration for inhibition of skolin-stimulated adenylate cyclase in cell line expressing human 5-hydroxytryptamine 1F receptor
- ChEMBL_29307 (CHEMBL640368) Binding affinity for adenosine A1 receptor using [3H]- CHA or [3H]- PIA antagonism of adenylate cyclase inhibition in rat adipocytes
- ChEBML_60524 Dopamine agonist (Dopamine receptor D1) activity was measured as increase in cAMP formation relative to maximum increase in dopamine-sensitive adenylate cyclase
- ChEMBL_31440 (CHEMBL873058) Compound was evaluated for the inhibition constant for inhibition of 8-lysine-vasopressin stimulated adenylate cyclase of pig kidney medullary membrane
- ChEMBL_31441 (CHEMBL645313) Compound was evaluated for the inhibition constant for inhibition of 8-lysine-vasopressin stimulated adenylate cyclase of pig kidney medullary membrane
- ChEBML_84894 In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
- ChEMBL_1673 (CHEMBL616664) Ability to inhibit forskolin-stimulated adenylate cyclase activity in Chinese hamster ovary (CHO) stable cell lines expressing human 5-hydroxytryptamine 1D receptor
- ChEMBL_30418 (CHEMBL645972) Binding affinity towards human adenosine A2B receptor in VA13 fibroblasts as inhibition of adenylate cyclase at 10 uM; Less than 10% inhibition
- ChEMBL_31723 (CHEMBL646262) Ability of the Compound to activate Adenylate cyclase activity was measured by the conversion of [alpha-32P]ATP to 3'5'-cyclic AMP
- ChEMBL_33481 (CHEMBL649812) Agonistic potency at alpha 2-Adrenergic receptor for inhibition of 10 uM forskolin-elicited stimulation of adenylate cyclase in human platelet membranes
- ChEMBL_58157 (CHEMBL672680) Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity
- ChEMBL_86248 (CHEMBL698014) Agonistic potency at alpha 2-Adrenergic receptor for inhibition of 10 uM forskolin-elicited stimulation of adenylate cyclase in human platelet membranes
- ChEMBL_106325 (CHEMBL709896) Stimulation of adenylate cyclase in HEK293 cells expressing the human MC4R receptor was determined by measuring cAMP accumulation using the RPA559 SPA assay
- ChEMBL_198197 (CHEMBL799125) Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells
- ChEMBL_201049 (CHEMBL803826) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1D-beta receptor in CHO-K1 cells
- ChEMBL_201050 (CHEMBL803827) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1D-beta receptor in CHO-K1 cells
- ChEBML_58154 Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
- ChEMBL_58154 (CHEMBL672898) Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 60% of dopamine maximum effect.
- ChEMBL_60526 (CHEMBL674937) Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes. Partial agonist, maximum effect 59% of dopamine maximum effect
- ChEMBL_361234 (CHEMBL871296) Binding affinity to rat pituitary GnRH receptor
- ChEBML_59628 Low binding affinity for dopamine receptor D2 from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol in bovine anterior pituitary membranes
- ChEMBL_59628 (CHEMBL670820) Low binding affinity for dopamine receptor D2 from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol in bovine anterior pituitary membranes
- ChEMBL_1468343 (CHEMBL3412222) Agonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
- ChEMBL_1468345 (CHEMBL3412224) Agonist activity at human 5HT1A receptor expressed in HEK293 cells assessed as cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
- ChEMBL_1934689 (CHEMBL4480341) Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assay
- ChEMBL_2289180 Inhibition of mouse glutaminyl cyclase
- ChEMBL_446074 (CHEMBL895169) Inhibition of oxidosqualene cyclase
- ChEMBL_519215 (CHEMBL946654) Inhibition of oxidosqualene cyclase
- ChEMBL_59487 (CHEMBL670139) High binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol in bovine anterior pituitary membranes
- ChEMBL_59626 (CHEMBL670818) Low binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol in bovine anterior pituitary membranes
- ChEMBL_59627 (CHEMBL670819) Low binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol in bovine anterior pituitary membranes
- ChEBML_2037 Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 0.24-0.55
- ChEMBL_198198 (CHEMBL799817) Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 110-250
- ChEMBL_198199 (CHEMBL799818) Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 50-550
- ChEMBL_607 (CHEMBL615476) Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-HT 1A receptor in HeLa cells; value ranges from 85-370
- ChEMBL_608 (CHEMBL615477) Compound was tested for its ability to inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1A receptor in HeLa cells; value ranges from 95-320
- ChEMBL_502057 (CHEMBL981268) Inhibition of rabbit muscle adenylate kinase
- ChEMBL_2281071 Inhibition of islet amyloid polypeptide (unknown origin) aggregation
- ChEMBL_2037 (CHEMBL616871) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 0.24-0.55
- ChEMBL_2038 (CHEMBL616872) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 0.6-2.0
- ChEMBL_2039 (CHEMBL616873) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 2.8-6.5
- ChEMBL_2040 (CHEMBL616838) Compound was tested for its ability inhibit forskolin-stimulated activity of adenylate cyclase coupled to human 5-hydroxytryptamine 1D receptor beta in CHO-K1 cells; value ranges from 30-70
- ChEMBL_2380513 Inhibition of human adenylate cyclase 2 expressed in ACdelta 3/6 knockout HEK293 cells assessed as cyclic AMP accumulation incubated for 30 min followed by FSK stimulation by HTR-FRET assay
- ChEMBL_686764 (CHEMBL1291003) Inhibition of 5-lipoxygenase activating protein
- ChEMBL_827630 (CHEMBL2049709) Inhibition of ubiquitin-activating enzyme E1
- ChEMBL_71868 (CHEMBL858403) Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
- ChEMBL_1874822 (CHEMBL4376111) Inhibition of mouse glutaminyl cyclase
- ChEMBL_2480328 Inhibition of glutaminyl cyclase (unknown origin)
- ChEMBL_907756 (CHEMBL3065679) Inhibition of Pisum sativum (pea) adenylate deaminase
- ChEMBL_1468344 (CHEMBL3412223) Antagonist activity at human 5HT7 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
- ChEMBL_1468346 (CHEMBL3412225) Antagonist activity at human 5HT1A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP concentration at 10'-6 M by adenylate cyclase activity based HTRF assay relative to control
- ChEMBL_321251 (CHEMBL881786) Inhibitory concentration against platelet activating factor receptor
- ChEBML_193173 Ability to release growth hormone in a rat pituitary cell assay
- ChEBML_59312 Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2
- ChEBML_71734 Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
- ChEBML_31732 Antagonistic activity evaluated in adenylyl cyclase assay
- ChEMBL_452980 (CHEMBL902125) Inhibition of Pneumocystis carinii oxidosqualene cyclase
- ChEMBL_452981 (CHEMBL902126) Inhibition of Saccharomyces cerevisiae oxidosqualene cyclase
- ChEMBL_556115 (CHEMBL956674) Inhibition of 2,3-oxidosqualene-lanosterol cyclase
- ChEBML_32050 Competitive inhibitory constant with Rat adenylate kinase II isozyme
- ChEBML_32222 Competitive inhibitory constant with Rat adenylate kinase M isozyme
- ChEMBL_31886 (CHEMBL645676) Inhibition of recombinant human E-type adenylate deaminase
- ChEMBL_32211 (CHEMBL875019) Competitive Inhibitory constant with Rat adenylate kinase IIl
- ChEMBL_907759 (CHEMBL3065682) Inhibition of Oryctolagus cuniculus (rabbit) muscle adenylate deaminase
- ChEBML_173122 In vitro growth hormone release was determined in rat pituitary cell assay
- ChEBML_71456 Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
- ChEBML_71737 Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
- ChEMBL_178770 (CHEMBL784303) Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
- ChEMBL_193174 (CHEMBL798749) Tested for GH-releasing property using classical rat pituitary cell assay
- ChEMBL_367962 (CHEMBL871111) Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
- ChEMBL_367963 (CHEMBL871112) Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
- ChEBML_151696 Compound was evaluated for anti-platelet activating factor potency
- ChEMBL_990534 (CHEMBL2447077) Inhibition of platelet activating factor receptor (unknown origin)
- ChEBML_213257 Inhibitory concentration against type V Adenyl Cyclase enzyme
- ChEMBL_148907 (CHEMBL756144) Inhibition against rat liver Oxidosqualene-lanosterol cyclase
- ChEMBL_1660125 (CHEMBL4009737) Inhibition of iso glutaminyl cyclase (unknown origin)
- ChEMBL_514281 (CHEMBL979111) Inhibition of human recombinant soluble adenylyl cyclase
- ChEBML_28549 Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor
- ChEMBL_302874 (CHEMBL828788) Inhibition constant against luciferase with respect to luciferyl-adenylate
- ChEMBL_32050 (CHEMBL644150) Competitive inhibitory constant with Rat adenylate kinase II isozyme
- ChEMBL_907754 (CHEMBL3065677) Inhibition of Bos taurus (calf) intestinal mucosa adenylate deaminase
- ChEMBL_1669006 (CHEMBL4018894) Effect on pancreatic polypeptide-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as pancreatic polypeptide pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 10.2 +/- 0.1 No_unit)
- ChEMBL_71455 (CHEMBL685984) Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
- ChEMBL_71456 (CHEMBL685985) Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
- ChEMBL_71728 (CHEMBL680407) Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
- ChEMBL_71737 (CHEMBL680260) Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
- ChEMBL_92942 (CHEMBL706153) Inhibition of L-type calcium channels in GH-3 rat pituitary cells
- ChEBML_148884 Inhibitory concentration against purified rat liver Oxidosqualene cyclase (OSC)
- ChEBML_148900 Inhibitory activity against Oxidosqualene-lanosterol cyclase in pig liver
- ChEMBL_149030 (CHEMBL759505) Inhibition constant against rat liver Oxidosqualene-lanosterol cyclase
- ChEMBL_149035 (CHEMBL874645) Tested for Oxidosqualene-lanosterol cyclase inhibition in rat
- ChEMBL_213256 (CHEMBL821464) Inhibitory concentration against Type V Adenyl Cyclase enzyme
- ChEMBL_213257 (CHEMBL821465) Inhibitory concentration against type V Adenyl Cyclase enzyme
- ChEMBL_2347559 Inhibition of human glutaminyl cyclase assessed as inhibition constant
- ChEMBL_79 (CHEMBL615200) In vitro inhibition of human 2,3-oxidosqualene cyclase.
- ChEMBL_80 (CHEMBL615201) In vitro inhibition of human 2,3-oxidosqualene cyclase.
- ChEMBL_28548 (CHEMBL640327) Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor
- ChEBML_100139 Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
- ChEMBL_100002 (CHEMBL710527) Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
- ChEMBL_207855 (CHEMBL810063) Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells
- ChEBML_155162 Inhibition of platelet activating factor (PAF) by binding to PAF receptor
- ChEBML_164923 Inhibition of rabbit platelet aggregation induced by platelet activating factor (PAF)
- ChEMBL_1555330 (CHEMBL3769214) Positive allosteric modulation of platelet-activating factor receptor (unknown origin)
- ChEMBL_322381 (CHEMBL856245) Inhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulation
- ChEBML_32046 Ability to inhibit rat adenylate kinase II, activity expressed as Inhibition constant
- ChEBML_32217 Non-competitive/Competitive inhibitory constant of compound with Rat adenylate kinase IIl
- ChEMBL_32200 (CHEMBL648979) Competitive binding inhibition constant of rat Adenylate kinase III was determined
- ChEMBL_32201 (CHEMBL648980) Competitive binding inhibition constant of rat adenylate kinase IIl was determined
- ChEMBL_32204 (CHEMBL648983) Non competitive binding inhibition of rat adenylate kinase IIl was determined
- ChEMBL_32216 (CHEMBL649601) Non-competitive inhibitory constant of compound with Rat adenylate kinase IIl
- ChEMBL_32221 (CHEMBL873064) Competitive Inhibitory constant of compound with Rat adenylate kinase M isozyme
- ChEMBL_32226 (CHEMBL646738) Noncompetitive inhibitory constant of compound with Rat adenylate kinase M isozyme
- ChEMBL_148881 (CHEMBL753756) Inhibitory concentration against purified rat liver Oxidosqualene cyclase (OSC)
- ChEMBL_148884 (CHEMBL753759) Inhibitory concentration against purified rat liver Oxidosqualene cyclase (OSC)
- ChEMBL_148889 (CHEMBL758670) Tested for Oxidosqualene-lanosterol cyclase inhibition in Pneumocystis carinii
- ChEMBL_148892 (CHEMBL758673) Tested for Oxidosqualene-lanosterol cyclase inhibition in Trypanosoma brucei
- ChEMBL_148893 (CHEMBL758674) Tested for Oxidosqualene-lanosterol cyclase inhibition in Trypanosoma brucei
- ChEMBL_148894 (CHEMBL758675) Tested for Oxidosqualene-lanosterol cyclase inhibition in Trypanosoma cruzi
- ChEMBL_148895 (CHEMBL758676) Tested for Oxidosqualene-lanosterol cyclase inhibition in Trypanosoma cruzi
- ChEMBL_148896 (CHEMBL758677) Tested for Oxidosqualene-lanosterol cyclase inhibition in Trypanosoma cruzi
- ChEMBL_201950 (CHEMBL809137) Inhibitory activity against squalene hopene cyclase from Alicyclobacillus acidocaldarius
- ChEMBL_305824 (CHEMBL829566) Inhibition of adenylyl cyclase activity in rat cortical membranes
- ChEMBL_2028546 (CHEMBL4682704) Antagonist activity at PAC1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of PACAP-induced inhibition of CREB phosphorylation preincubated for 30 mins followed by PACAP stimulation and measured after 30 mins by Western blot analysis
- ChEMBL_2221684 (CHEMBL5135018) Antagonist activity at PAC-1 receptor (unknown origin) expressed in CHO cells assessed as inhibition of PACAP-induced increase in intracellular cAMP level pretreated for 30 mins followed by PACAP stimulation measured after 1 hr by cAMP-Glo assay
- ChEMBL_200340 (CHEMBL806572) Dissociation constant binding to somatostatin receptor of At-20 mouse pituitary carcinoma cell membranes
- ChEMBL_357594 (CHEMBL871314) Activity at human GHS-R1a receptor in rat pituitary cells assessed as GH release
- ChEMBL_71729 (CHEMBL680408) Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
- ChEMBL_155133 (CHEMBL764095) Inhibition of [3H]PAF binding to human platelet activating factor receptor
- ChEMBL_155144 (CHEMBL760185) Displacement of [3H]-WEB 2086 from Platelet activating factor receptor (PAF)
- ChEMBL_155162 (CHEMBL760201) Inhibition of platelet activating factor (PAF) by binding to PAF receptor
- ChEMBL_155163 (CHEMBL761901) Inhibition of platelet activating factor(PAF) by binding to PAF receptor
- ChEMBL_4307 (CHEMBL618416) Inhibition of 5-lipoxygenase activating protein using human leukocyte membrane preparations
- ChEBML_32036 Ability to inhibit Escherichia coli adenylate kinase II, activity expressed as Inhibition constant
- ChEBML_32228 Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of AMP
- ChEMBL_32217 (CHEMBL649602) Non-competitive/Competitive inhibitory constant of compound with Rat adenylate kinase IIl
- ChEMBL_32224 (CHEMBL646736) Non-competitive Inhibitory constant of compound with Rat adenylate kinase M isozyme
- ChEMBL_32225 (CHEMBL646737) Non-competitive inhibitory constant of compound with Rat adenylate kinase M isozyme
- ChEBML_148909 Inhibitory activity against Oxidosqualene-lanosterol cyclase enzyme obtained from rat liver
- ChEMBL_148897 (CHEMBL754981) Inhibitory activity against Oxidosqualene-lanosterol cyclase from human liver microsomes
- ChEMBL_148911 (CHEMBL756148) Inhibitory activity against Oxidosqualene-lanosterol cyclase from Rat liver microsomes
- ChEMBL_37258 (CHEMBL650173) Percent adenylyl cyclase activation at 10000 nM of compound concentration
- ChEMBL_38297 (CHEMBL647101) Percent adenylyl cyclase activation at 10000 nM of compound concentration
- ChEMBL_452982 (CHEMBL902127) Inhibition of human oxidosqualene cyclase expressed in Pichia pastoris cells
- ChEMBL_87 (CHEMBL827084) Concentration required to inhibit rat liver 2,3-oxidosqualene-lanosterol cyclase
- ChEBML_100017 Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
- ChEBML_71423 In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
- ChEBML_71439 In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
- ChEBML_71726 Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
- ChEMBL_100140 (CHEMBL712498) Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
- ChEMBL_210510 (CHEMBL811905) Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.
- ChEMBL_210511 (CHEMBL811906) Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells
- ChEMBL_326849 (CHEMBL860444) Displacement of [3H]spiperone from human dopamine D2(short) receptor in rat pituitary GH4C1 cells
- ChEMBL_447480 (CHEMBL896503) Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
- ChEMBL_72506 (CHEMBL685171) Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand
- ChEBML_155153 Displacement of [3H]ligand from platelet activating factor (PAF) receptor in rabbit platelets
- ChEBML_155157 Tested for inhibition of [3H]PAF binding to rabbit Platelet activating factor receptor
- ChEBML_4306 Compound was tested for its binding activity towards 5-lipoxygenase activating protein (FLAP)
- ChEBML_4310 Tested for inhibition of leukotriene biosynthesis by binding to 5-lipoxygenase activating protein
- ChEBML_32198 Ability to inhibit rat adenylate kinase III, activity expressed as Inhibition constant; Competitive inhibition
- ChEMBL_32065 (CHEMBL644163) Non-competitive/Competitive inhibitory constant of compound with Rat adenylate kinase II isozyme
- ChEMBL_32202 (CHEMBL648981) Competitive inhibition of adenylate kinase III in rat liver with respect to ATP
- ChEMBL_32228 (CHEMBL645747) Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of AMP
- ChEMBL_32231 (CHEMBL645750) Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of ATP
- ChEBML_58207 In vitro ability to inhibit [3H]spiperone binding to Dopamine receptor D2 from pig anterior pituitary tissue
- ChEBML_59178 Ability to displace [3H]spiperone binding from anterior pituitary Dopamine receptor D2 in the absence of GTP
- ChEMBL_100017 (CHEMBL709254) Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
- ChEMBL_100143 (CHEMBL857595) Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
- ChEMBL_166183 (CHEMBL770867) Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
- ChEMBL_361237 (CHEMBL871299) Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
- ChEMBL_71726 (CHEMBL680405) Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
- ChEBML_148886 Concentration for the inhibition of rat microsomal oxidosqualene cyclase-lanosterol synthase (OSC)
- ChEMBL_148908 (CHEMBL756145) Inhibition of compound was measured on rat microsomal Oxidosqualene-lanosterol cyclase
- ChEMBL_149027 (CHEMBL756415) Binding affinity towards competitive inhibition against rat microsomal Oxidosqualene-lanosterol cyclase
- ChEMBL_88 (CHEMBL615208) Concentration required to inhibit rat liver 2,3-oxidosqualene-lanosterol cyclase (OSC)
- ChEBML_154992 Inhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog blood
- ChEBML_155151 Binding affinity for Platelet Activating Factor receptor using [3H]PAF in rabbit platelet membranes
- ChEBML_155155 In vitro intrinsic binding affinity at platelet activating factor receptor using rabbit platelet membranes
- ChEMBL_307258 (CHEMBL830837) Inhibition of [3H]PAF binding to platelet activating factor receptor in human platelet
- ChEMBL_4306 (CHEMBL618415) Compound was tested for its binding activity towards 5-lipoxygenase activating protein (FLAP)
- ChEMBL_303537 (CHEMBL839650) Ability to displace [3H]spiperone from human Dopamine receptor D2S stably transfected in GH4C1 (rat pituitary) cells
- ChEMBL_58207 (CHEMBL672778) In vitro ability to inhibit [3H]spiperone binding to Dopamine receptor D2 from pig anterior pituitary tissue
- ChEMBL_59178 (CHEMBL672642) Ability to displace [3H]spiperone binding from anterior pituitary Dopamine receptor D2 in the absence of GTP
- ChEMBL_59486 (CHEMBL670138) High binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol
- ChEMBL_59625 (CHEMBL670961) Low binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol
- ChEMBL_63343 (CHEMBL679285) Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.
- ChEMBL_71736 (CHEMBL680259) Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
- ChEMBL_842141 (CHEMBL2091558) Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
- ChEMBL_32047 (CHEMBL644147) Competitive binding inhibition constant (Ki) of rat adenylate kinase (AK II) isozymes was determined
- ChEMBL_32048 (CHEMBL644148) Competitive binding inhibition constant(Ki) of rat adenylate kinase (AK II) isozymes was determined
- ChEMBL_32054 (CHEMBL644153) Inhibitory activity against rat adenylate kinase II was determined in the presence of ATP
- ChEMBL_32057 (CHEMBL644155) Inhibitory activity against rat adenylate kinase II was determined in the presence of AMP
- ChEMBL_32198 (CHEMBL648977) Ability to inhibit rat adenylate kinase III, activity expressed as Inhibition constant; Competitive inhibition
- ChEMBL_32199 (CHEMBL648978) Ability to inhibit rat adenylate kinase III, activity expressed as Inhibition constant; Competitive inhibition
- ChEMBL_514924 (CHEMBL972650) Inhibition of adenylate binding site of Photuris pennsylvanica luciferase by quantitative high throughput screening
- ChEMBL_514925 (CHEMBL972651) Inhibition of adenylate binding site of Photinus pyralis luciferase by quantitative high throughput screening
- ChEMBL_1668991 (CHEMBL4018879) Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide induced-calcium flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 0.1 nM)
- ChEBML_201951 Inhibitory activity against squalene hopene cyclase from Alicyclobacillus acidocaldarius expressed in Escherichia coli
- ChEMBL_149028 (CHEMBL759503) Binding affinity towards non-competitive inhibition against rat microsomal Oxidosqualene-lanosterol cyclase
- ChEBML_154987 Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation
- ChEMBL_155148 (CHEMBL760189) In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets
- ChEMBL_155151 (CHEMBL760191) Binding affinity for Platelet Activating Factor receptor using [3H]PAF in rabbit platelet membranes
- ChEMBL_162884 (CHEMBL768980) Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.
- ChEMBL_4313 (CHEMBL618421) Binding affinity of compound for 5-lipoxygenase activating protein protein by FLAP binding assay
- ChEMBL_819515 (CHEMBL2033320) Displacement of [125I]L-691,831 from 5-lipoxygenase-activating protein in human polymorphonuclear cells
- ChEBML_58366 Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
- ChEMBL_2033594 (CHEMBL4687752) Agonist activity at GHSR in Wistar rat pituitary gland cells assessed as induction of GH release by RIA
- ChEBML_32194 Ability to inhibit Escherichia coli adenylate kinase III, activity expressed as Inhibition constant; Non competitive inhibition
- ChEMBL_1340550 (CHEMBL3254974) Competitive inhibition of Sprague-Dawley rat liver adenylate kinase 2 by Lineweaver-Burk plot analysis
- ChEMBL_1340551 (CHEMBL3254975) Competitive inhibition of Sprague-Dawley rat liver adenylate kinase 3 by Lineweaver-Burk plot analysis
- ChEMBL_32062 (CHEMBL644160) Non competitive binding inhibition constant (Ki) of rat adenylate kinase (AK II) isozymes was determined
- ChEMBL_32063 (CHEMBL644161) Non competitive binding inhibition constant(Ki) of rat adenylate kinase (AK III) isozymes was determined
- ChEMBL_32229 (CHEMBL645748) Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of AMP competitive inhibition
- ChEMBL_32233 (CHEMBL645752) Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of ATPnon competitive inhibition
- ChEBML_30292 Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor
- ChEMBL_1341454 (CHEMBL3253174) Inhibition of dopamine-sensitive rat brain adenylyl cyclase activity assessed as cAMP level
- ChEMBL_1447042 (CHEMBL3374948) Inhibition of human GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
- ChEMBL_1447044 (CHEMBL3374950) Inhibition of rat GPR119 activity by homogeneous time resolved fluorescence cyclase (cAMP) assay
- ChEMBL_148883 (CHEMBL753758) Compound was evaluated for the binding affinity against rat liver oxidosqualene cyclase (OSC)
- ChEMBL_148888 (CHEMBL758669) Compound was tested for inhibition of purified Oxidosqualene-lanosterol cyclase from Candida albicans
- ChEMBL_148898 (CHEMBL882413) Compound was tested for inhibition of purified Oxidosqualene-lanosterol cyclase from pig liver
- ChEMBL_148906 (CHEMBL756760) Compound was tested for inhibition of purified Oxidosqualene-lanosterol cyclase from rat liver
- ChEMBL_2311751 Inhibition of human glutaminyl cyclase activity assessed as fluorescence using H-Gln-AMC substrate
- ChEMBL_46466 (CHEMBL657913) Compound was tested for inhibition of Adenylyl cyclase in cannabinoid receptor 1 (CB1).
- ChEMBL_46994 (CHEMBL658963) Compound was tested for inhibition of Adenylyl cyclase in cannabinoid receptor 2 (CB2).
- ChEMBL_1669017 (CHEMBL4018905) Positive allosteric modulation of human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide induced-calcium flux by measuring pancreatic polypeptide pEC50 at 30 uM treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay (Rvb = 10 +/- 0.04 No_unit)
- ChEBML_154997 Inhibition of platelet-activating factor receptor binding activity in dog platelets using [3H]-PAF as radioligand.
- ChEMBL_154987 (CHEMBL882497) Inhibition of the binding of [3H]C18-Platelet activating factor to human platelet membrane preparation
- ChEMBL_155146 (CHEMBL760187) Inhibiting Platelet activating factor receptor by radioreceptor binding assay using rabbit platelets and [3H]-PAF
- ChEMBL_1621549 (CHEMBL3863832) Antagonist activity at PAR4 (unknown origin) assessed as inhibition of activating peptide-induced receptor activation
- ChEMBL_965439 (CHEMBL2395085) Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs
- ChEMBL_2125418 (CHEMBL4834763) Inhibition of islet amyloid polypeptide (unknown origin) aggregation after 24 hrs by thioflavin T based fluorescence assay
- ChEMBL_611538 (CHEMBL1066382) Displacement of [125I]Pancreatic polypeptide from human neuropeptide Y4 receptor in human HEK293 cells after 40 mins
- ChEBML_225775 Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol
- ChEBML_71605 Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
- ChEMBL_50973 (CHEMBL666691) Effective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell cultures
- ChEMBL_58366 (CHEMBL672803) Concentration required to inhibit 50% dopamine receptor D2 in a cell free homogenate of intermediate lobe of pituitary gland
- ChEMBL_59310 (CHEMBL666963) Ability to displace [3H]spiperone binding from anterior pituitary Dopamine receptor D2 in the presence of 100 uM GTP
- ChEBML_32055 Inhibitory activity against rat adenylate kinase II was determined in the presence of ATP, non competitive inhibition
- ChEMBL_32051 (CHEMBL644151) Inhibitory activity against rat adenylate kinase II was determined in the presence of AMP, competitive inhibition
- ChEMBL_32056 (CHEMBL644154) Inhibitory activity against rat adenylate kinase II was determined in the presence of ATP, competitive inhibition
- ChEMBL_32230 (CHEMBL645749) Inhibitory activity against rat Adenylate kinase M isoenzyme in the presence of AMP non competitive inhibition
- ChEBML_218131 Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
- ChEBML_92 Compound was evaluated for inhibitory activity against 2,3-oxidosqualene-lanosterol cyclase in rat liver microsomes
- ChEMBL_145690 (CHEMBL753316) Inhibition of Forskolin-Stimulated Adenylyl Cyclase in CHO cells expressing Opioid receptor kappa 1
- ChEMBL_148879 (CHEMBL753754) Compound concentration that cause 50% inhibition of pig liver oxidosqualene cyclase (OSC) was determined
- ChEMBL_148904 (CHEMBL756758) Compound was tested for kinetic inhibition constant against Oxidosqualene-lanosterol cyclase from pig liver
- ChEMBL_149029 (CHEMBL759504) Compound was tested for kinetic inhibition constant against Oxidosqualene-lanosterol cyclase from rat liver
- ChEMBL_514280 (CHEMBL979110) Inhibition of Spirulina platensis adenylyl cyclase assessed as cAMP level by cAMP immunogenic assay
- ChEMBL_589681 (CHEMBL1057686) Inhibition of human glutaminyl cyclase expressed in Pichia pastoris by pGAP coupled enzyme assay
- ChEBML_162869 Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP)
- ChEMBL_154997 (CHEMBL767101) Inhibition of platelet-activating factor receptor binding activity in dog platelets using [3H]-PAF as radioligand.
- ChEMBL_155145 (CHEMBL760186) Displacement of [3H]-WEB 2086 from Platelet activating factor receptor (guinea pig) transgenic mouse muscle membrane
- ChEMBL_27877 (CHEMBL640575) In vitro inhibitory activity against human Jurkat T-Cells stably transfected with activating transcription factor 1
- ChEMBL_1994888 (CHEMBL4628783) Inhibition of SET7 (unknown origin) using biotinylated histone polypeptide as substrate in presence of SAM by AlphaLISA assay
- ChEMBL_100131 (CHEMBL858015) Inhibition of the in vitro binding of [125I]-labeled leuprolide to the rat pituitary luteinizing hormone releasing hormone (LHRH) receptor.
- ChEMBL_210509 (CHEMBL811904) Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol
- ChEMBL_225775 (CHEMBL847681) Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol
- ChEMBL_59583 (CHEMBL672934) In vitro binding affinity towards dopamine receptor was determined in bovine anterior pituitary membrane using [3H]dihydroergocriptine as the radioligand
- ChEMBL_71605 (CHEMBL689137) Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
- ChEMBL_71606 (CHEMBL689138) Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
- ChEMBL_71731 (CHEMBL680410) Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
- ChEMBL_1669003 (CHEMBL4018891) Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of pancreatic polypeptide-induced arrestin 3 recruitment by measuring pancreatic polypeptide EC50 at 30 uM after 30 mins by BRET assay (Rvb = 5.6 nM)
- ChEMBL_1669021 (CHEMBL4018909) Positive allosteric modulation of human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cells assessed as potentiation of pancreatic polypeptide-induced arrestin 3 recruitment by measuring pancreatic polypeptide pEC50 at 30 uM after 30 mins by BRET assay (Rvb = 8.3 +/- 0.12 No_unit)
- ChEMBL_29907 (CHEMBL641978) Inhibitory activity against rat Adenylate kinase M isoenzyme was determined in the presence of ATP, Competitive inhibition
- ChEMBL_32052 (CHEMBL873039) Inhibitory activity against rat adenylate kinase II was determined in the presence of AMP, non competitive inhibition
- ChEMBL_32055 (CHEMBL874426) Inhibitory activity against rat adenylate kinase II was determined in the presence of ATP, non competitive inhibition
- ChEMBL_32058 (CHEMBL644156) Inhibitory activity against rat adenylate kinase II was determined in the presence of AMP, non competitive inhibition
- ChEMBL_145021 (CHEMBL857697) In vitro inhibitory activity of the compound against rat microsomal 2,3-Oxidosqualene lanosterol cyclase (OSC)
- ChEMBL_148890 (CHEMBL758671) Compound was tested for inhibition of solubilized and partially purified Saccharomyces cerevisiae Oxidosqualene-lanosterol cyclase
- ChEMBL_148899 (CHEMBL754982) Compound was tested for inhibition of solubilized and partially purified pig liver Oxidosqualene-lanosterol cyclase
- ChEMBL_1753283 (CHEMBL4188043) Inhibition of human glutaminyl cyclase using Gln-AMC as substrate by pGAPase coupled fluorescence assay
- ChEMBL_218131 (CHEMBL822565) Effective concentration for stimulation of adenylyl cyclase activity in CHO-beta3 AR expressing cell membranes
- ChEMBL_38798 (CHEMBL652339) Evaluated for Adenylyl cyclase activation as % of the maximal stimulation with isoproterenol at 100 nM
- ChEMBL_684953 (CHEMBL1286368) Antagonist activity at human cloned 5HT6 receptor expressed in human HeLa cells by cyclase assay
- ChEMBL_1766330 (CHEMBL4201577) Displacement of [3H]AVP from V1B receptor in Wistar rat pituitary membranes incubated for 60 mins by microplate scintillation counting method
- ChEMBL_458712 (CHEMBL942047) Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation
- ChEMBL_562461 (CHEMBL1010964) Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
- ChEMBL_63360 (CHEMBL679124) Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
- ChEMBL_71754 (CHEMBL680276) Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
- ChEMBL_97295 (CHEMBL879809) Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
- ChEMBL_97296 (CHEMBL711951) Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
- ChEBML_154999 In vitro for platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets.
- ChEBML_177423 Inhibitory activity expressed as the concentration required to inhibit platelet-activating factor (PAF) induced maximum aggregation by 50%
- ChEMBL_1456351 (CHEMBL3368360) Inhibition of human cardiac slowly activating delayed rectifier K+ channel expressed in CHO cells by electrophysiology assay
- ChEMBL_1463477 (CHEMBL3399887) Inhibition of non-activated Erk2 (unknown origin) using activating Mek1 and peptide substrate by coupled Erk2 assay
- ChEMBL_1621532 (CHEMBL3863815) Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
- ChEMBL_1621541 (CHEMBL3863824) Antagonist activity at PAR1 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response
- ChEMBL_1621542 (CHEMBL3863825) Antagonist activity at PAR1 in human platelets assessed as inhibition of activating peptide-induced P-selectin activation
- ChEMBL_162869 (CHEMBL767230) Inhibition of platelet aggregation using Adenosine diphosphate (ADP) as activating agent in rabbit platelet rich plasma (PRP)
- ChEMBL_89718 (CHEMBL696421) Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma (PRP)
- ChEMBL_89719 (CHEMBL696422) Inhibition of platelet aggregation using adenosine diphosphate (ADP) as activating agent in human platelet rich plasma PRP
- ChEMBL_29908 (CHEMBL642753) Inhibitory activity against rat Adenylate kinase M isoenzyme was determined in the presence of ATP, non competitive inhibition
- ChEBML_60521 Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
- ChEMBL_104609 (CHEMBL712996) Effective concentration against human MT2 (Melatonin) receptor stably expressed in NIH3T3 cells in adenylyl cyclase assay
- ChEMBL_145020 (CHEMBL753716) In vitro inhibitory activity of the compound against rat microsomal 2,3-Oxidosqualene cyclase-Lanosterol synthase (OSC)
- ChEMBL_1552649 (CHEMBL3762588) Partial agonist activity at delta opioid receptor (unknown origin) assessed as inhibition of adenylyl cyclase activity
- ChEMBL_329339 (CHEMBL863562) Activity at adrenergic alpha-2B receptor expressed in opposum kidney OK cell by adenylyl cyclase assay
- ChEMBL_89 (CHEMBL615209) Evaluated for its activity to inhibit rat liver 2,3-oxidosqualene-lanosterol cyclase, activity expressed as Ki
- ChEBML_58209 Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as low affinity state
- ChEMBL_100135 (CHEMBL712414) In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
- ChEMBL_100147 (CHEMBL712504) In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
- ChEMBL_34974 (CHEMBL649503) Inhibitory concentration against [125 I]Ang II binding to rat pituitary membranes Angiotensin II receptor type 1 without 0.2% bovine serum albumin
- ChEMBL_58210 (CHEMBL669940) Compound was evaluated for the ability to displace [3H]spiperone at dopamine receptor in porcine anterior pituitary gland as high affinity state
- ChEBML_1654002 Inhibition of CHK1 (unknown origin) using polypeptide substrate after 40 mins in presence of [gamma-33P]ATP by scintillation counting method
- ChEBML_1654003 Inhibition of CHK2 (unknown origin) using polypeptide substrate after 40 mins in presence of [gamma-33P]ATP by scintillation counting method
- ChEMBL_1554146 (CHEMBL3769118) Inhibition of human recombinant GSK3-beta using prephosphorylated polypeptide as substrate incubated for 30 mins by Glo-type luminescence assay
- ChEMBL_2342334 Inhibition of recombinant human BACE1 using fluorogenic polypeptide Mca-SEVNLDAEFRK(Dpn)RRNH2 as substrate incubated for 60 mins by FRET assay
- ChEMBL_151699 (CHEMBL760448) Antagonist activity against platelet activating factor (PAF) receptor in rabbit platelet membranes using [3H]C18-PAF as radioligand
- ChEMBL_151707 (CHEMBL760600) Ability to displace [3H]PAF from its Platelet Activating Factor (PAF) receptor in rabbit platelet membrane in vitro.
- ChEMBL_155143 (CHEMBL760184) In vitro inhibition of [3H]-C18 PAF binding to human platelet membrane Platelet activating factor receptor was determined
- ChEMBL_1582061 (CHEMBL3817138) Inhibition of EGFR exon19 deletion activating mutant autophosphorylation in human PC9 cells incubated for 2 hrs by ELISA
- ChEMBL_158347 (CHEMBL768491) Binding potency against Platelet activating factor (PAF) receptor using [3H]C18-PAF as radioligand on rabbit platelet membranes
- ChEMBL_177423 (CHEMBL784402) Inhibitory activity expressed as the concentration required to inhibit platelet-activating factor (PAF) induced maximum aggregation by 50%
- ChEMBL_1933878 (CHEMBL4479530) Antagonist activity against PAR4 activating peptide domain in in human platelets assessed as inhibition of P-selectin activation
- ChEMBL_32053 (CHEMBL644152) Inhibitory activity against rat adenylate kinase II was determined in the presence of AMP, competitive and non competitive inhibition
- ChEMBL_100146 (CHEMBL712503) In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
- ChEMBL_554185 (CHEMBL963642) Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
- ChEMBL_58205 (CHEMBL672776) Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as high affinity state
- ChEMBL_58208 (CHEMBL672779) Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as high affinity state
- ChEMBL_58209 (CHEMBL669939) Compound was evaluated for the ability to displace [3H]spiperone at Dopamine receptor D2 in porcine anterior pituitary gland as low affinity state
- ChEMBL_145691 (CHEMBL753317) Inhibition of forskolin-stimulated adenylyl cyclase activity by compound in CHO cells expressing Opioid receptor kappa 1
- ChEMBL_329336 (CHEMBL863559) Activity at 5HT7 receptor expressed in human corneal epithelial CEPI-17-CL4 cells by adenylyl cyclase assay
- ChEMBL_329337 (CHEMBL863560) Activity at adrenergic alpha-2A receptor expressed in human clonic adenocarcinoma HT29 cell by adenylyl cyclase assay
- ChEMBL_60521 (CHEMBL674932) Inhibition of Dopamine receptor D1 activity by functional cyclase assay using cell free homogenate of rat striatum
- ChEMBL_1676257 (CHEMBL4026400) Inhibition of BACE-1 (unknown origin) using APP derived polypeptide harboring Lys-Met/Asn-Leu mutation as substrate by FRET assay
- ChEBML_158835 Ability to inhibit platelet activating factor (PAF) binding to platelets by 50% was determined by using [3H]PAF as radioligand
- ChEBML_4308 Measuring the affinity of leukotriene synthesis inhibitor for 5-Lipoxygenase activating protein (FLAP) by using [125I]L-691831 as radioligand.
- ChEBML_4312 The compound was tested for the inhibition of binding of [125I]- L- 691,831 binding to 5-lipoxygenase activating protein (FLAP)
- ChEMBL_1436962 (CHEMBL3389021) Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
- ChEMBL_154984 (CHEMBL765337) In vitro effect on inhibition of the binding of [3H]C18-Platelet activating factor to human PMN membranes preparation
- ChEMBL_155140 (CHEMBL759830) Compound was evaluated for inhibition of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptor
- ChEMBL_158397 (CHEMBL767061) Molar concentration required to inhibit 50% of the activating delayed-rectifier K+ current in isolated guinea pig ventricular myocytes
- ChEMBL_1855338 (CHEMBL4356067) Inhibition of VPS4B (unknown origin) assessed as reduction in ATPase activity in presence of activating fragment of substrate CHMP1B
- ChEMBL_4309 (CHEMBL618417) Measuring the affinity of leukotriene synthesis inhibitor for 5-lipoxygenase activating protein by using [125I]L-691831 as radioligand.
- ChEMBL_980993 (CHEMBL2427714) Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
- ChEMBL_29909 (CHEMBL642754) Inhibitory activity against rat adenylate kinase II (AK-II) isoenzyme was determined in the presence of ATP, non competitive inhibition
- ChEMBL_625913 (CHEMBL1115139) Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
- ChEMBL_71732 (CHEMBL680411) Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
- ChEBML_27925 Inhibition of stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via A2 adenosine receptor in human platelet membranes
- ChEBML_38913 Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
- ChEMBL_1712259 (CHEMBL4122308) Inhibition of human glutaminyl cyclase using Gln-AMC as substrate in presence of pyroglutamyl peptidase by fluorometric assay
- ChEMBL_329340 (CHEMBL863564) Activity at adrenergic Alpha-2C receptor expressed in rat-mouse hybrid NH108-15 cell by adenylyl cyclase assay
- ChEMBL_72643 (CHEMBL686062) Inhibitory activity against guanylate cyclase coupled receptor binding site in rabbit lung by using [125I]-ANP-(103-126)
- ChEMBL_154998 (CHEMBL767102) Compound tested in vitro for Platelet activating factor receptor antagonist activity in a binding assay using washed whole dog platelets
- ChEMBL_155001 (CHEMBL764538) Compound was evaluated for inhibitory activity of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptor
- ChEMBL_4312 (CHEMBL618420) The compound was tested for the inhibition of binding of [125I]- L- 691,831 binding to 5-lipoxygenase activating protein (FLAP)
- ChEMBL_100133 (CHEMBL712412) The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
- ChEMBL_458546 (CHEMBL942804) Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
- ChEMBL_2196606 (CHEMBL5109122) Inhibition of recombinant human GSK-3beta using prephosphorylated polypeptide substrate measured after 30 mins in presence of ATP by Kinase-Glo Luminescent assay
- ChEMBL_1463789 (CHEMBL3404799) Agonist activity at human S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
- ChEMBL_1463791 (CHEMBL3404801) Agonist activity at mouse S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
- ChEMBL_1463793 (CHEMBL3404803) Agonist activity at rat S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
- ChEMBL_1463795 (CHEMBL3404805) Agonist activity at dog S1P1 receptor assessed as change in cAMP level by homogeneous time resolved fluorescence cyclase assay
- ChEMBL_1471049 (CHEMBL3420494) Agonist activity at human recombinant adenosine A2A receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
- ChEMBL_1471050 (CHEMBL3420495) Agonist activity at human recombinant adenosine A2B receptor transfected in CHO cells assessed as induction of adenylyl cyclase activity
- ChEMBL_2151037 (CHEMBL5035499) Inhibition of human recombinant glutaminyl cyclase using H-Gln-AMC hydrobromide as substrate measured after 15 mins by fluorimetry
- ChEMBL_38913 (CHEMBL652016) Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO Beta-3 adrenergic receptor cell membrane.
- ChEMBL_38915 (CHEMBL652018) Compound was tested for its ability to stimulate adenylyl cyclase activity in CHO-beta-3 adrenergic receptor cell membrane.
- ChEMBL_461292 (CHEMBL927311) Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity
- ChEMBL_1933876 (CHEMBL4479528) Antagonist activity against PAR4 activating peptide domain in human platelets assessed as inhibition of alpha2bbeta3 activation level by PAC1 binding assay
- ChEMBL_599342 (CHEMBL1043683) Displacement of [35S]-labeled ligand from VLA4 in human Jurkat cells washed with buffer containing activating Mn2+ by competitive binding assay
- ChEMBL_34975 (CHEMBL884036) Inhibitory concentration against specific binding of [125 I]Ang II to rat pituitary membranes (Angiotensin II receptor, type 1) in presence of 0.2% bovine serum albumin
- ChEMBL_1722005 (CHEMBL4137005) Inhibition of BACE1 (1 to 454 residues) (unknown origin) using APP derived polypeptide harboring Lys-Met/Asn-Leu mutation as substrate by FRET assay
- ChEMBL_2081048 (CHEMBL4736839) Inhibition of recombinant human GSK-3beta using phosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay
- ChEMBL_2148329 (CHEMBL5032727) Inhibition of human recombinant GSK-3beta using prephosphorylated polypeptide as substrate incubated for 30 mins in presence of ATP by Kinase-Glo luminescence assay
- ChEMBL_2214647 (CHEMBL5127779) Inhibition of WEE1 (unknown origin) using LSNLYHQGKFLQTFCGSPLYRRR polypeptide as substrate incubated for 40 mins in presence of [gamma-33P]-ATP by scintillation counting method
- ChEMBL_755832 (CHEMBL1803566) Inhibition of human recombinant GSK3-beta using prephosphorylated polypeptide substrate after 30 mins by Glow-type luminescence assay in presence of 1 uM ATP
- ChEMBL_1668992 (CHEMBL4018880) Positive allosteric modulation of human C-terminal eYFP-fused human NY4 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide-mediated Ca2+ flux treated at 20 secs post baseline detection followed by addition of pancreatic polypeptide after 140 secs by Fluo2-AM fluorescent dye based-assay
- ChEMBL_1752777 (CHEMBL4187537) Inhibition of Lp-PLA2 in human plasma LDL fractions using 2-thio platelet-activating factor as substrate by TMB dye based spectrophotometry
- ChEMBL_599864 (CHEMBL1043647) Receptor occupancy of VLA4 in whole blood washed with buffer containing non activating Ca2+ and Mg2+ at 37 degC after 3 hrs
- ChEMBL_827633 (CHEMBL2050672) Inhibition of FLAG-tagged ubiquitin-activating enzyme E1 assessed as inhibition of GST-ubiquitin/FLAG-E1 intermediate formation by Western blot analysis
- ChEBML_38168 Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
- ChEBML_38789 Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
- ChEMBL_1274848 (CHEMBL3090422) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_1452898 (CHEMBL3366214) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_1467364 (CHEMBL3411601) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
- ChEMBL_27926 (CHEMBL642334) Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.
- ChEMBL_30863 (CHEMBL646360) Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via Adenosine A2 receptor in rat PC12 membranes
- ChEMBL_562993 (CHEMBL1015330) Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_566531 (CHEMBL955117) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_587705 (CHEMBL1037719) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity
- ChEMBL_598162 (CHEMBL1044346) Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay
- ChEMBL_598759 (CHEMBL1040174) Agonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as induction of adenylyl cyclase activity by RIA
- ChEMBL_598761 (CHEMBL1040176) Antagonist activity at human cloned 5HT6 receptor expressed in HeLa cells assessed as inhibition of adenylyl cyclase activity by RIA
- ChEMBL_627568 (CHEMBL1113574) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_772801 (CHEMBL1837540) Antagonist activity human recombinant adenosine 2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_964094 (CHEMBL2394447) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_100009 (CHEMBL710694) The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
- ChEMBL_2213590 (CHEMBL5126722) Inhibition of human recombinant GSK3beta using prephosphorylated polypeptide GSM as substrate incubated for 30 mins in presence of ATP by Kinase-Glo Luminescent Kinase Assay
- ChEMBL_477686 (CHEMBL937483) Inhibition of human Kv1.5 channel expressed in mouse L929 cells assessed as blockade of ultra rapidly activating potassium current by voltage clamp technique
- ChEMBL_595740 (CHEMBL1045263) Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating Gq protein assessed as [3H]inositol phosphate production
- ChEBML_148880 Concentration that cause 50 percent inhibition of binding of [14C]-labeled (3S)-oxidosqualene to isolated rat liver oxidosqualene cyclase (OSC) was determined
- ChEBML_37241 Agonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nM
- ChEMBL_1471048 (CHEMBL3420493) Agonist activity at human recombinant adenosine A1 receptor transfected in CHO cells assessed as inhibition of forskolin-induced adenylyl cyclase activity
- ChEMBL_1549261 (CHEMBL3757839) Antagonist activity at human A2B adenosine receptor expressed in CHO cell membranes assessed as inhibition of NECA stimulated adenylyl cyclase activity
- ChEMBL_2347558 Inhibition of human recombinant glutaminyl cyclase using glutaminyl-7-amido-4-methylcoumarin as substrate assessed as inhibition constant by microplate reader analysis
- ChEMBL_313054 (CHEMBL835745) Inhibitory concentration required to reverse the dopamine inhibition of forskolin-stimulated adenyl cyclase activity in CHO cells stably expressing hD4 receptor
- ChEMBL_37243 (CHEMBL651564) Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
- ChEMBL_38168 (CHEMBL650239) Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
- ChEMBL_38789 (CHEMBL650698) Agonistic activity against the cloned human Beta-3 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
- ChEMBL_794134 (CHEMBL1931872) Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
- ChEMBL_100141 (CHEMBL712499) The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
- ChEMBL_1505783 (CHEMBL3595021) Antagonist activity at ghrelin receptor in Sprague-Dawley rat primary pituitary cells assessed as inhibition of ghrelin-induced growth hormone secretion incubated for 15 mins by ELISA method
- ChEMBL_2184379 (CHEMBL5096461) Inhibition of recombinant human GSK-3beta incubated for 30 mins using prephosphorylated polypeptide as substrate in presence of ATP by Kinase-Glo reagent based luminescent assay
- ChEBML_209247 Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
- ChEBML_86450 Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF.
- ChEMBL_599863 (CHEMBL1043646) Displacement of [35S]-labeled ligand from VLA4 in human Jurkat cells washed with buffer containing non activating Ca2+ and Mg2+ by competitive binding assay
- ChEMBL_148880 (CHEMBL753755) Concentration that cause 50 percent inhibition of binding of [14C]-labeled (3S)-oxidosqualene to isolated rat liver oxidosqualene cyclase (OSC) was determined
- ChEMBL_1563857 (CHEMBL3784463) Inhibition of human recombinant glutaminyl cyclase expressed in Escherichia coli using H-Gln-Gln-H substrate measured for 15 mins by spectrophotometry
- ChEMBL_37241 (CHEMBL651562) Agonist activity against cloned human beta-1 adrenergic receptor as percent activation of adenyl cyclase activity at a concentration of 1000 nM
- ChEMBL_583012 (CHEMBL1051850) Agonist activity at human 5HT4C receptor expressed in HEK293 cells assessed as accumulation of cAMP by flash plate adenylyl cyclase activation assay
- ChEMBL_807 (CHEMBL615786) Ability to inhibit 5-HT sensitive,forskolin-stimulated adenylyl cyclase(FSC) activity in rat hippocampal membranes mediated through 5-hydroxytryptamine 1A receptor
- ChEMBL_966260 (CHEMBL2395921) Inhibition of human glutaminyl cyclase expressed in HEK293 cells using L-glutaminyl-beta-naphthylamine as substrate after 1 hr by fluorometric analysis
- ChEMBL_1714128 (CHEMBL4124177) Inhibition of recombinant human JAK3 (781 to 1124 residues) expressed in baculovirus expression system assessed as reduction in polypeptide substrate phosphorylation in presence of ATP by ELISA
- Enzymatic Activity of Human Glutaminyl Cyclase In Vitro During studies of the effect of Compounds I-X, which are the object of the present invention, on the enzymatic activity of glutaminyl cyclase in vitro, the direct inhibitory effect of Compounds I-X on recombinant intracellular human glutaminyl cyclase first has been found. The glutaminyl cyclase activity at various concentrations of Compounds I-X has been studied at 25 C. with the use of a fluorescent substrate L-glutaminyl 2-naphthyl amide (Gln-bNA) (Anal Biochem. 2002 Apr. 1; 303(1):49-56). The reaction mixture having a volume of 100-μl has contained 50 μM of fluorogenic substrate; 0.2 units of human pyroglutaminyl aminopeptidase (1 unit is defined as an amount hydrolyzing 1 micromole of pGlu-bNA per minute), and an aliquot of the recombinant intracellular human glutaminyl cyclase (gQC) in 50 mM trisaminomethane-HCl and 5% glycerol, a pH is 8.0. The reaction was initiated by adding to the reaction mixture an aliquot of glutaminyl cyclase incubated with Compounds I-X for 5 minutes.
- ChEMBL_124502 (CHEMBL733338) Tested in vitro for filter plate binding versus gamma-[33P]ATP in active recombinant murine FLAG-P38 alpha fusion protein (GST-Activating transcription factor-2).
- ChEMBL_1436868 (CHEMBL3387790) Antagonist activity at platelet-activating factor receptor in human PMNs assessed as inhibition of PAF-induced intracellular Ca2+ release by fluorescence based calcium flux assay
- ChEMBL_1655135 (CHEMBL4004501) Inhibition of human KCNQ1/KCNE1 expressed in HEK293 cells assessed as reduction in slowly activating delayed rectifier cardiac potassium current by patch clamp electrophysiology method
- ChEMBL_209247 (CHEMBL815534) Antagonistic activity against thrombin receptor, inhibition of secreted radiolabeled [3H]5-HT from washed human platelets stimulated by 3 uM thrombin receptor activating peptide (TRAP)
- ChEMBL_819516 (CHEMBL2033321) Inhibition of 5-lipoxygenase-activating protein in human polymorphonuclear cells assessed as inhibition of calcium ionophore-induced LTB4 production in presence of human whole blood
- ChEMBL_2129834 (CHEMBL4839263) Inhibition of human soluble adenylyl cyclase assessed as reduction in cAMP levels in the presence of alpha-32p labeled ATP by biochemical assay
- ChEMBL_2240293 (CHEMBL5154189) Inhibition of mouse PDE9A expressed in recombinant CHO cells coexpressing soluble guanylate cyclase incubated for 6 mins by [3H]-cGMP scintillation proximity assay
- ChEMBL_1655138 (CHEMBL4004504) Inhibition of human ERG expressed in CHOK1 cells assessed as reduction in rapidly activating delayed rectifier cardiac potassium current by whole-cell voltage-patch clamp assay
- ChEMBL_500566 (CHEMBL971431) Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
- ChEMBL_500569 (CHEMBL971434) Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay
- ChEMBL_595741 (CHEMBL1045264) Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production
- ChEMBL_595742 (CHEMBL1045265) Agonist activity at human P2Y6 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating Gq protein assessed as [3H]inositol phosphate production at 10 uM
- ChEMBL_978590 (CHEMBL2422107) Inhibition of human glutaminyl cyclase expressed in Escherichia coli DH5alpha using H-Gln-AMC as substrate by fluorometric analysis in presence of pyroglutamyl aminopeptidase
- ChEBML_1643866 Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEBML_1643867 Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEBML_1643868 Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEMBL_1292705 (CHEMBL3123572) Binding affinity to human recombinant adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity after 20 mins
- ChEMBL_1471051 (CHEMBL3420496) Antagonist activity at human recombinant adenosine A3 receptor transfected in CHO cells assessed as reversal of NECA-induced inhibition of forskolin-induced adenylyl cyclase activity
- ChEMBL_1701169 (CHEMBL4052151) Agonist activity at recombinant human adenosine A2A receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
- ChEMBL_1701170 (CHEMBL4052152) Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity by [alpha-32P]ATP assay
- ChEMBL_1822665 (CHEMBL4322429) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
- ChEMBL_1822666 (CHEMBL4322430) Antagonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity by Glo-sensor cAMP assay
- ChEMBL_2019975 (CHEMBL4673788) Antagonist activity at human A2B receptor expressed in CHO cell membrane assessed as reduction in NECA-stimulated adenylyl cyclase activity in presence of [alpha32P]ATP
- ChEMBL_2289172 Inhibition of human glutaminyl cyclase using L-glutamine-7-amido-4-methylcoumarin as substrate incubated for 10 mins in presence of pyroglutamyl peptidase by fluorometry analysis
- ChEMBL_959780 (CHEMBL2383352) Agonist activity at CB1 receptor in mouse Neuro2a cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 15 mins by liquid scintillation spectrophotometry
- ChEMBL_1643866 (CHEMBL3992795) Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEMBL_1643867 (CHEMBL3992796) Agonist activity at human DOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEMBL_1643868 (CHEMBL3992797) Agonist activity at human KOR expressed in HEK293 cells assessed as inhibition of forskolin-induced adenylyl cyclase-mediated cAMP accumulation after 30 mins by HTRF assay
- ChEMBL_1677776 (CHEMBL4027919) Agonist activity at recombinant human adenosine A1 receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
- ChEMBL_1677777 (CHEMBL4027920) Agonist activity at recombinant human adenosine A2B receptor expressed in CHO cell membranes assessed as stimulation of adenylyl cyclase activity in presence of [alpha-31P]ATP
- ChEMBL_959779 (CHEMBL2383351) Agonist activity at human CB2 receptor transfected in CHO cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 15 mins by liquid scintillation spectrophotometry
- ChEMBL_1676259 (CHEMBL4026402) Inhibition of recombinant human GSK3beta using prephosphorylated polypeptide as substrate preincubated for 30 mins followed by addition of kinase-glo stop solution measured after 10 mins by Kinase-Glo luminescence assay
- ChEMBL_1784113 (CHEMBL4255630) Inhibition of recombinant human full length N-terminal GST-tagged GSK-3beta expressed in Sf9 insect cells using prephosphorylated polypeptide as substrate after 30 mins by kinase-Glo reagent based luminescence assay
- ChEMBL_1677782 (CHEMBL4027925) Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase in presence of [alpha-31P]ATP
- ChEMBL_1802980 (CHEMBL4275272) Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay
- ChEMBL_46617 (CHEMBL658203) Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
- ChEMBL_46833 (CHEMBL657302) Effective concentration for inhibition of human Cannabinoid receptor 2-mediated adenylyl cyclase using African green monkey (COS-7) cells transfected with the cDNA of human CB2 receptor
- ChEMBL_684759 (CHEMBL1285786) Agonist activity at recombinant PTHR1 expressed in HEK293 cells co-transfected with CRE-Luc assessed as increase of adenylyl cyclase activity after 4.5 hrs by luciferase assay
- Enzymatic Activity of Human Glutaminyl Cyclase In Vitro The glutaminyl cyclase activity at various concentrations of Compounds I-X has been studied at 25 C. with the use of a fluorescent substrate L-glutaminyl 2-naphthyl amide (Gln-bNA) (Anal Biochem. 2002 Apr. 1; 303(1):49-56). The reaction mixture having a volume of 100-μl has contained 50 μM of fluorogenic substrate; 0.2 units of human pyroglutaminyl aminopeptidase (1 unit is defined as an amount hydrolyzing 1 micromole of pGlu-bNA per minute), and an aliquot of the recombinant intracellular human glutaminyl cyclase (gQC) in 50 mM trisaminomethane-HCl and 5% glycerol, a pH is 8.0. The reaction was initiated by adding to the reaction mixture an aliquot of glutaminyl cyclase incubated with Compounds I-X for 5 minutes.
- ChEMBL_1803885 (CHEMBL4276177) Inhibition of human recombinant N-terminal His6-tagged human GSK-3beta expressed in Baculovirus infected SF9 cells using prephosphorylated-GS2 polypeptide as substrate after 30 mins by kinase-Glo reagent based luminescence assay
- ChEMBL_2324055 Positive allosteric modulation of human Y4 receptor transfected with COS-7 cells co-transfected with delta6Galphaqi4-myr assessed as potentiation of pancreatic polypeptide EC20 response measured after 240 secs by calcium 2+ flux assay
- ChEMBL_2347560 Inhibition of N-terminal his6-tagged human recombinant glutaminyl cyclase expressed in Escherichia coli using H-Gln-AMC as substrate incubated for 60 mins in presence of pyroglutamyl peptidase
- ChEMBL_910805 (CHEMBL3057561) Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min
- ChEMBL_1799138 (CHEMBL4271430) Inhibition of human recombinant Rad6B using ubiquitin and histone H2A and ubiquitin-activating enzyme E1 preincubated for 1 hr before ubiquitin and histone H2A addition by SDS-PAGE and immunoblotting analysis
- ChEMBL_1291661 (CHEMBL3119408) Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins in presence of [alpha-32P]ATP
- ChEMBL_1736932 (CHEMBL4152682) Antagonist activity at recombinant human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced adenylyl cyclase activity after 20 mins by [alpha-32P]ATP assay
- ChEMBL_2014889 (CHEMBL4668467) Allosteric inhibition of SHP2 (unknown origin) using DiFMUP as substrate preincubated for 60 mins in presence of activating peptide IRS-1 followed by substrate addition and measured after 60 mins by fluorescence method
- ChEMBL_1591035 (CHEMBL3831120) Antagonist activity at recombinant human adenosine A2B receptor expressed in CHOK1 cell membrane assessed as inhibition of NECA-stimulated adenylyl cyclase activity incubated for 20 mins in presence of [alpha32P]ATP
- ChEMBL_1701164 (CHEMBL4052146) Agonist activity at recombinant human adenosine A1 receptor expressed in CHO cell membranes assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 mins in presence of [alpha-32P]ATP
- ChEMBL_1621530 (CHEMBL3863813) Antagonist activity at PAR4 in human platelets assessed as inhibition of activating peptide-induced PAC1 binding response preincubated for 20 mins followed by agonist addition for 20 mins by FITC-based flow cytometric analysis
- ChEMBL_2014890 (CHEMBL4668468) Allosteric inhibition of SHP2 (unknown origin) using DiFMUP as substrate preincubated for 30 mins in presence of activating peptide [IRSl_pY1172(dPEG8)pY1222] followed by substrate addition and measured over 30 mins by fluorescence method
- ChEMBL_2324059 Displacement of K22-[TAMRA]-Nle-17,30-PP from human Nluc-tagged Y4R transfected with COS-7 cells assessed as inhibition constant of pancreatic polypeptide incubated for 5 mins followed by substrate addition by NanoBRET assay (Rvb = 2.7 nM )
- ChEMBL_1660123 (CHEMBL4009735) Inhibition of mouse glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 mins followed by enzyme addition by pGAPase coupled fluorometry
- ChEMBL_1660124 (CHEMBL4009736) Inhibition of human glutaminyl cyclase assessed as reduction in conversion of H-Gln-AMC hydrobromide to pGlu-AMC preincubated with substrate for 10 mins followed by enzyme addition by pGAPase coupled fluorometry
- ChEMBL_1701172 (CHEMBL4052154) Antagonist activity at recombinant human adenosine A3 receptor expressed in CHO cell membranes assessed as reversal of NECA-mediated inhibition of adenylyl cyclase activity after 10 mins by [alpha-32P]ATP assay
- ChEMBL_2211768 (CHEMBL5124717) Binding affinity to N-terminal His6/Sumo-tagged NSD2 PWWP1 domain (211 to 350 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) using ATKAARKSAPATGGV-Lys (me)2-KPHRYRPG polypeptide as substrate incubated for 3 hrs by HTRF assay
- In Vitro Assay Preparation of working solution: 2×Glutaminyl Cyclase substrate was diluted in assay buffer to 5 M. 2×enzyme solution and QPCTL was diluted in assay buffer to 0.8 nM. Glutaminyl Cyclase Developer was diluted in assay buffer to 1×(containing 10 mM 1-Benzyl-Imidazole). Serial dilution of test compounds was performed in DMSO. The final DMSO concentration in 100 μl reaction was 1%. The assay buffer was 50 mM Tris, pH 8.0, 0.01% BSA.Procedure: 50 μL of 2×Glutaminyl Cyclase substrate solution was added into the assay plate followed by 50 μL of 2×enzyme solution. The plate was centrifuged for 1 min at 1000 rmp. Next the plate was incubated for 45 minutes at 37° C. This was followed by the additional of 50 μL of the prepared Glutaminyl Cyclase developer and incubated for additional 30 min at 37° C. Results were read on SpectraMax Paradigm detecting with emission at Ex/Em=490 nm/520 nm.
- ChEMBL_2129836 (CHEMBL4839265) Inhibition of human soluble adenylyl cyclase transfected (4-4 clones)in human HEK293 cells assessed as reduction in cAMP levels preincubated for 5 mins with test compounds in the presence of IBMX by ELISA
- ChEMBL_2034409 (CHEMBL4688567) Inhibition of recombinant human N-terminal His6-tagged GSK3beta H350L mutant expressed in baculovirus infected Sf21 cells using prephosphorylated polypeptide as substrate incubated for 1 min followed by substrate addition and measured after 30 mins by Kinase-Glo luminescence assay
- ChEMBL_2014887 (CHEMBL4668465) Allosteric inhibition of full-length His6-tagged human SHP2 (2 to 527 residues) expressed in Escherichia coli using DiFMUP as substrate in presence of activating peptide (LN(pY)IDLDLV(dPEG8)LST(pY)ASINFQK-amide) by fluorescence method
- ChEMBL_2148637 (CHEMBL5033035) Agonist activity at full length TLX activating element expressed in human HEK293T cells coexpressing human full-length TLX/Gal4-VP 16 assessed as decrease in reporter activity at 100 uM by luciferase reporter gene assay relative to control
- ChEMBL_1669007 (CHEMBL4018895) Effect on neuropeptide Y-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as neuropeptide Y pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 7.9 +/- 0.2 No_unit)
- ChEMBL_1669008 (CHEMBL4018896) Effect on peptide YY-mediated displacement of 125I-pancreatic polypeptide from human C-terminal eYFP-tagged NY4 receptor expressed in HEK293 cell membranes assessed as peptide YY pKi at 30 uM after 5 hrs by by scintillation counting (Rvb = 8 +/- 0.2 No_unit)
- ChEMBL_1874814 (CHEMBL4376103) Inhibition of recombinant human N-terminal His6-tagged glutaminyl cyclase (Ala33 to Leu361 residues) expressed in baculovirus infected Sf21 insect cells using H-Gln-AMC hydrobromide as substrate measured in presence of pGAPase by fluorometric assay
- CSNK1A1 Assay 1 Inhibitory activity of compounds of the present invention in presence of 1 μM adenosine-tri-phosphate (ATP) was quantified employing the CSNK1A1 assay as described in the following paragraphs. In essence, the enzyme activity is measured by quantification of the adenosine-di-phosphate (ADP), which is generated as a co-product of the enzyme reaction, via the “ADP-Glo™ Kinase Assay” kit from the company Promega. This detection system works as follows: In a first step the ATP not consumed in the kinase reaction is quantitatively converted to cAMP employing an adenylate cyclase (“ADP-Glo-reagent”), then the adenylate cyclase is stopped and the ADP generated in the kinase reaction converted to ATP which generates in a luciferase-based reaction a glow-luminescence signal (“Kinase Detection Reagent”). Recombinant fusion protein of N-terminal Glutathion-S-Transferase (GST) and full-length human CSNK1A1, expressed by baculovirus infected insect cells and purified via Glutathion affinity chromatography, was purchased from Life Technologies (product no. PV4174) and used as enzyme. As substrate for the kinase reaction the biotinylated peptide Btn-Ahx-SGSEGDSESGEEEG (C-terminus in amide form) was used which can be purchased e.g. from the company Biosyntan (Berlin-Buch, Germany).
- Functional Assay A functional assay screen for the inhibition of adenylate cyclase (AC) activity was chosen as the subsequent assay. This screen would allow us to gain a better understanding of the intrinsic activity of the analogues that displayed moderate to high sub-micromolar affinity for the CBRs. Reaching full-receptor occupancy, which is predicted to produce maximal efficacy, is desirable at 10 μM concentration of all the compounds was used. The non-selective CB1R/CB2R full agonist CP-55,940 was used as a positive control and it produced 45% AC-inhibition at CB1Rs endogenously expressed in Neuro2A cells (FIG. 19A) and 37% AC-inhibition in CHO cell transfected with hCB2 receptors (FIG. 19B). Most compounds tested exhibit AC-inhibition similar to that produced by the full agonist CP-55,940. TV-5-129, TV-6-249, and TV-6-41, however, produce lower AC-inhibition at CB1Rs than the full agonist CP-55,940 with −4, 18, and 16% inhibition, respectively (FIG. 19A). Despite little or no AC-inhibition observed at CB1Rs, these compounds behaved differently at CB2Rs. Specifically, the three compounds in question exhibited AC-inhibition that was in the range of the inhibition seen with CP-55,940 and were shown to inhibit adenylate cyclase with 22.1, 33.2, and 20.8%, respectively (FIG. 19B).
- ChEMBL_1659128 (CHEMBL4008740) Agonist activity at human dopamine D2 receptor-short expressed in CHO-K1 cells assessed as reduction in adenylyl cyclase activator NKH 477 induced cAMP accumulation preincubated for 10 mins followed by NKH 477 addition by HTRF assay
- Late stage assay provider results from the probe development effort to identify inhibitors of plasma platelet activating factor acetylhydrolase (pPAFAH) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Providers: Brian Bahnson (Univ. of Delaware); Benjamin Cravatt, (TSRI) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1R01HL084366 Grant Proposal PI: Brian Bahnson External Assay ID: pPAFAH_INH_FLUO_GELBASEDABPP_3XIC50_HTSHITS Name: Late stage assay provider results from the probe development effort to identify inhibitors of plasma platelet activating factor acetylhydrolase (pPAFAH): fluorescence-based dose response biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) assay for HTS compounds. Description: This project aims to develop specific inhibitors of plasma platelet activating factor acetylhydrolase (pPAFAH), and three associated members of the serine hydrolase family of enzymes-PAFAH2, PAFAH1b2, and PAFAH1b3. pPAFAH, an enzyme linked to the inflammatory
- ChEMBL_2014886 (CHEMBL4668464) Allosteric inhibition of full length N-terminal His6-tagged human SHP2 (2 to 593 residues) expressed in Escherichia coli using DiFMUP as substrate in presence of activating peptide preincubated for 60 mins followed by substrate addition amd measured after 30 mins by fluorescence method
- Assay of Full-Length SHP2 Phosphatase Activity Assay 1. Reagents and MaterialsHuman full-length SHP2 recombinant protein: BPS Bioscience, Cat #79018;SHP2 substrate DiFMUP (1 mM): BPS Bioscience, Cat #79769;SHP2 activating peptide (100 μM): BPS Bioscience, Cat #79319-2;DTT: Merck, Cat #DTT-RO;384-well plate: Corning, Cat #3575;96-well plate: Thermo Fisher Scientific, Cat #249952;Instrument: EnVision 2104, PerkinElmer.2. Preparation of Reaction SolutionsThe test compound was dissolved in DMSO and diluted with DMSO to 100.0 μM, and the compound was further 3-fold diluted with DMSO to: 100.00, 33.33, 11.11, 3.70, 1.23, 0.41, 0.14 and 0.05 μM. Then 4 μL of the compound at different dilution concentrations was added to 96 μL of an enzymatic reaction buffer to prepare a 4× test compound, wherein DMSO was at the concentration of 4% (DMSO was at the final concentration of 1%).Preparation of 1× enzymatic reaction buffer: the 5× reaction buffer (250 mM HEPES, 500 mM NaCl, 2.5 mM EDTA, 0.005% Brij-35 and 0.01% BSA, pH 7.2) was diluted 5-fold with deionized water, and then DTT was added thereto so that the 1× enzymatic reaction buffer contained 5 mM DTT.Preparation of 4× mixed solution of SHP2 enzyme/activating peptide: the SHP2 enzyme (75.5 nM) and activating peptide (100 μM) were diluted with the enzymatic reaction buffer to prepare a 4× mixed solution of SHP2 enzyme/activating peptide (0.12 nM SHP2 and 2 μM activating peptide), so that the SHP2 enzyme and activating peptide were at the final concentrations of 0.03 nM and 0.5 μM in the enzymatic reaction system, respectively.Preparation of 2×DiFMUP substrate: 1 mM DiFMUP was diluted 100-fold with the enzymatic reaction buffer to prepare a 2× substrate (10 μM), so that the substrate DiFMUP was at the final concentration of 5 μM in the enzymatic reaction system.
- ChEMBL_2441539 Inhibition of recombinant C-terminal truncated human SHP2 (1 to 530 residues) using 6,8-difluoro-4-methylumbelliferyl phosphate as substrate and H2N-LN(pY)IDLDLV-(PEG)8-LST(pY)ASINFQK-amide as activating peptide preincubated for 30 mins followed by substrate addition and measured over 30 mins by fluorescence based analysis
- TrkB Enzyme Assay TrkB kinase activity was measured against its ability to phosphorylate synthetic tyrosine residues within a generic polypeptide substrate using homogeneous time-resolved fluorescence (HTRF) technology. Reaction products are detected with the addition of strepavidin-linked and phosphotyrosine-specific antibodies using the Tecan Ultra Evolution microplate fluorometer after additional 3 h incubation at room temperature.
- sAC Biochemical Cyclase Assay Assays for sAC activity using purified protein were performed in 100 ul reactions containing 4 mM MgCl2, 2 mM CaCl2, 1 mM ATP, 40 mM NaHCO3, 50 mM Tris pH 7.5, and 3 mM DTT. Each reaction contained 1,000,000 counts of alpha-32P labeled ATP. Generated cAMP was purified using sequential Dowex and Alumina chromatography.
- RF-MSS cyclase assay The RapidFire 365 High-throughput MS System (Agilent Technologies; RF-MSS) can process samples every 15 seconds allowing analysis of a 384 well plate in under two hours; thus, RF-MSS provides a platform for high throughput MS screening which can simultaneously measure both cAMP produced and ATP consumed in an individual sAC assay. Using the RF-MSS we observed no appreciable sample carryover between assay samples, and we were able to detect both a sAC-dependent increase in cAMP signal (FIG. 2A) and decrease in ATP signal (FIG. 2B) over time. When measured in the presence of increasing concentrations of substrate ATP in the presence of Mg2+ as the sole divalent cation, HCO3 − stimulated sAC activity by increasing the Vmax with little effect on the apparent Km for substrate ATP-Mg2+ (FIG. 2C). Addition of Ca2+ stimulated sAC activity by decreasing its apparent Km for ATP, and addition of both Ca2+ and HCO3 − synergistically activated sAC. These data confirm that using RF-MSS as a tool for measuring in vitro adenylyl cyclase activity is comparable to the known, radioactivity based, two-column method for measuring adenylyl cyclase activity.
- ChEMBL_1668994 (CHEMBL4018882) Positive allosteric modulation of human C-terminal eYFP-fused human NY2 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 10 +/- 0.1 No_unit)
- ChEMBL_1668995 (CHEMBL4018883) Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)