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T38782 |
Mant-GTPγS
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Mant-GTPγS, an effective GTP analog, displays strong competitive inhibition of adenylyl cyclase (AC). Additionally, it acts as a potent inhibitor of YdeH. |
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T82252 |
GTPγS tetralithium
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GTPγS (tetralithium) is a G-protein activator known for its role in preventing proteolytic degradation of proteins, facilitating tyrosine kinase-dependent GLUT4 translocation, stimulating phospholipases, and promoting ac... |
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T10639 |
C-021 dihydrochloride
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CCR
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C-021 dihydrochloride is a potent CCR4 antagonist. It potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM. |
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T21870 |
C-021
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4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy- |
CCR
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C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s ... |
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T2036 |
6-OAU
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GTPL5846 |
GPR
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6-OAU (GTPL5846)(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay. |
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T4407 |
SR17018
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Opioid Receptor
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SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM. |
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TQ0108 |
MK-6892
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GPR
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MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM). |
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T37075 |
CB2R PAM
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Ec2la |
Cannabinoid Receptor
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CB2R PAM is an orally active cannabinoid type 2 receptor (CB2Rs) positive mutational modulator that enhances CP 55940 and 2-Arachidonylglycerol-stimulated [35S]GTPγS binding to CB2 receptors, but has no effect in the abs... |
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T7316 |
LY2828360
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Cannabinoid Receptor
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LY2828360 is a cannabinoid (CB) receptor 2 agonist (Ki = 40.3 nM). It selectively activates CB2 over CB1 in a GTPγS binding assay (EC50s = 20.1 and >100,000 nM, respectively). |
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T41231 |
GP 1a
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Cannabinoid Receptor
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PERK
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Arrestin
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GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and incr... |
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T37610 |
AT-121
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Opioid Receptor
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AT-121 is a dual μ-opioid and neuropeptide receptor partial agonist (Kis 16.49 and 3.67 nM, respectively). It stimulates [35S]GTPγS binding to cell membranes expressing either μ-opioid receptors or neuropeptide receptors... |
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T26869 |
BMS-986122
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BMS 986122 |
Opioid Receptor
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BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC5... |
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T21935L |
AMN082 free base
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AMN082 |
GluR
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AMN082 free base is a metabotropic glutamate receptor 7 allosteric agonist. |
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T6923 |
Ozanimod
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RPC-1063 |
S1P Receptor
,
LPL Receptor
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Ozanimod (RPC-1063) (RPC1063) is a specific oral S1P Receptor 1 modulator. Ozanimod has been used in trials studying the treatment of Crohn's Disease, Ulcerative Colitis, Multiple Sclerosis, and Relapsing Multiple Sclero... |
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T32341 |
JWH-251
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JWH 251, a cannabimimetic indole, has a high affinity tothe central cannabinoid (CB1) receptor (Ki = 29 nM) and a comparatively modest affinity for the peripheral cannabinoid (CB2) receptor (Ki = 146 nM). JWH 251 can st... |
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T67760 |
JNJ-65355394
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Others
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JNJ-65355394 is an effective O-GlcNAc hydrolase (OGA) inhibitor and an OGA chemical probe. |
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T26667 |
ASN04421891
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ASN 04421891,ASN-04421891 |
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ASN04421891 is a potent GPR17 receptor modulator, with an EC 50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 is promising to be used for neurodegenerative diseases research[1]. |
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T62918 |
GPR84 antagonist 3
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GPR84 Antagonist 3 (compound 42), a potent inhibitor of the G-protein-coupled receptor 84 (GPR84), exhibits a pIC50 value of 8.28, indicating strong antagonistic activity by inhibiting GTPγS. Additionally, it possesses a... |
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T74993 |
A3AR modulator 1
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A3AR modulator 1 (MRS8054), an orally active positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) (Adenosine Receptor), significantly enhances the efficacy (E max) of Cl-IB-MECA-stimulated [35 S]GTPγS ... |
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T62756 |
LY487379
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LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). lY487379 enhances glutamate-stimulated [35 S] GTPγS binding to mGlu2 receptors (EC50: 1.7 μM) and mGlu3 receptors (EC50>10 μM). lY487379 induces c... |
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T75907 |
Ac-RYYRIK-NH2 TFA
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Ac-RYYRIK-NH2 TFA acts as both a potent partial agonist for ORL1 when transfected in CHO cells (K d = 1.5 nM) and an endogenous ligand of ORL1. Moreover, it serves as a specific antagonist that inhibits G protein activat... |
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T21999 |
(±)-J 113397
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(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist (K(i): cloned human ORL1=1.8 nM). J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC 50... |
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T69798 |
4-Me-PDTic HCl
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4-Me-PDTic is a potent and selective Kappa Opioid Receptor Antagonist. 4-Me-PDTic had a Ke = 0.37 nM in a [35S]GTPγS binding assay and was 645- and >8100-fold selective for the κ relative to the μ and δ opioid receptors,... |
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T35591 |
Guanfacine-13C,15N3
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Guanfacine-13C,15N3 |
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Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A... |
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T83685 |
UFP101 TFA
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UFP101 is a synthetic peptide that functions as an antagonist of the nociceptin receptor, demonstrating high affinity with a Ki of 0.06 nM in CHO cells expressing the human receptor. It exhibits selectivity for the nocic... |
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T36722 |
Deltorphin II (trifluoroacetate salt)
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Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [3... |
