|
T8423 |
ML417
|
|
Dopamine Receptor
,
Arrestin
|
|
ML417 is a selective and brain penetrant agonist of D3 Dopamine (EC50 : 38 nM). |
|
T26869 |
BMS-986122
|
BMS 986122 |
Opioid Receptor
|
|
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... |
|
T28073 |
MLS1547
|
MLS000051547,MLS 1547,MLS-1547 |
Dopamine Receptor
|
|
MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assa... |
|
T61562 |
CB1R Allosteric modulator 3
|
|
cAMP
,
Cannabinoid Receptor
|
|
CB1R Allosteric modulator 3 is a potent CB1R modulator.CB1R Allosteric modulator 3 inhibits cAMP and β-Arrestin, and can be used for the study of obesity and nicotine addiction. |
|
T23434 |
GPR35 agonist 2
|
TC-G 1001 |
GPR
,
Arrestin
|
|
GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively. |
|
T33452 |
ML192
|
ML-192,CID1434953,CID 1434953,ML 192,CID-1434953 |
Cannabinoid Receptor
,
GPR
,
Arrestin
|
|
ML192 (CID1434953) is a selective GPR55 ligand antagonist. ML192 is an inhibitor that inhibits β-arrestin transport, ERK1/2 phosphorylation, and PKCβII translocation. |
|
TP2158L1 |
TRV-120027 acetate (1234510-46-3 free base)
|
|
RAAS
,
Arrestin
|
|
TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling. |
|
TP2158 |
TRV-120027 TFA
|
TRV-120027 TFA (1234510-46-3 free base) |
RAAS
,
Arrestin
|
|
TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling. |
|
TP1923L1 |
ELA-14(human) acetate
|
ELA-14(human) acetate (1886973-05-2 free base) |
Apelin receptor
,
Arrestin
|
|
ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide. |
|
T4390 |
ML221
|
|
Apelin receptor
,
Arrestin
|
|
ML221 is a potent apelin /APJ functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays. |
|
T77673 |
7-FluorotryptaMine HCl
|
|
GPR
,
Arrestin
|
|
7-FluorotryptaMine HCl is a potent aromatic monoamine GPRC5A agonist that induces GPRC5A-mediated β-arrestin recruitment.7-FluorotryptaMine HCl can be used to study signalling pathways related to immunity and cancer. |
|
TP1922L1 |
ELA-11 (human) acetate(1784687-32-6 free base)
|
|
Apelin receptor
,
Arrestin
|
|
ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. |
|
TP2112L |
TC14012 acetate
|
TC14012 acetate(368874-34-4 free base) |
CXCR
,
Arrestin
|
|
TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrest... |
|
T41231 |
GP 1a
|
|
Cannabinoid Receptor
,
PERK
,
Arrestin
|
|
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... |
|
T33613 |
NCGC00135472
|
NCGC 00135472,DRV1 (GPR32) agonist C2A,C2A,NCGC-00135472 |
Others
|
|
NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1/GPR32 receptor in beta-blocker and cAMP assays ... |
|
T29065 |
UNC9994
|
UNC-9994,UNC 9994 |
|
|
UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities. |
|
T29061 |
UNC0006
|
UNC 0006,UNC-0006 |
|
|
UNC0006 is a β-arrestin-biased dopamine D2 ligand. |
|
T29066 |
UNC9995
|
UNC-9995,UNC 9995 |
|
|
UNC9995 is a β-Arrestin-Biased Dopamine D2 Receptor agonist (β-Arrestin, EC50 = 120 nM; Emax = 88%). |
|
T29064 |
UNC9975
|
UNC-9975 |
|
|
UNC9975 is an analog of aripiprazole and a β-arrestin-biased D2R agonist. |
|
T70040 |
BRD5814
|
|
|
|
BRD5814 is a highly brain penetrant β-arrestin biased D2R antagonist. |
|
T10926 |
CYT-1010
|
|
Others
|
|
CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively. |
|
T23866 |
CCX777
|
CCX 777,CCX-777 |
Arrestin
|
|
CCX777 is a partial agonist recruited to ACKR3 by β-arrestin-2 and is used in cancer research. |
|
T37304 |
5-OxoETE methyl ester
|
|
|
|
5-OxoETE methyl ester is an esterified form of the polyunsaturated keto acid 5-oxoETE . 5-OxoETE methyl ester is an agonist of oxoeicosanoid receptor 1 (OXER1; EC50 = 1.54 μM for β-arrestin recruitment) that has a higher... |
|
T62853 |
UNC9994 hydrochloride
|
|
|
|
UNC9994 hydrochloride is a functionally selective, β-arrestin-biased dopamine D2 receptor (D2R) agonist (Ki: 79 nM) that selectively activates β- arresttin recruitment and signal transduction. UNC9994 hydrochloride is a ... |
|
T79312 |
FGH31
|
|
Dopamine Receptor
|
|
FGH31 (Compound 24), a dopamine D4 agonist, exhibits potent and selective GRK2-dependency with a K i of 1.6 nM and partially activates β-arrestin [1]. |
|
T10926L |
CYT-1010 hydrochloride
|
|
Others
|
|
CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively. |
|
T79744 |
GPR55 agonist 4
|
|
|
|
GPR55 agonist 4 (Compound 28), with an EC50 of 131 nM for hGPR55 and 1.41 nM for rGPR55, effectively induces β-arrestin recruitment to human GPR55 [1]. |
|
T61964 |
RXFP3/4 agonist 2
|
|
RXFP receptor
|
|
RXFP3/4 agonist 2 is a potent non-peptidic bis-RXFP3/4 agonist that induces the interaction between RXFP3 and β-arrestin-2, and can be used to study diseases caused by metabolic abnormalities. |
|
T78735 |
D1R antagonist 1
|
|
Dopamine Receptor
|
|
Compound 12a (D1R antagonist 1) is a D1R antagonist that participates in both G-protein-coupled and β-arrestin-mediated signaling pathways [1]. |
|
T61371 |
CB1R Allosteric modulator 4
|
|
|
|
CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arresti... |
|
T80140 |
(Val3,Pro8)-Oxytocin
|
|
Oxytocin Receptor
|
|
(Val3,Pro8)-Oxytocin functions primarily as a Gq-dependent pathway agonist and exhibits secondary activity as a reduced efficacy agonist for β-arrestin recruitment and receptor-mediated endocytosis at the oxytocin recept... |
|
T78736 |
D3R ligand 1
|
|
Dopamine Receptor
|
|
D3R Ligand 1 (compound 23b) is a potent, selective antagonist of the dopamine D3 receptor (Ki=66 nM), incorporating a THPB template. It inhibits both G-protein- and β-arrestin-mediated signaling pathways [1]. |
|
TP1922 |
ELA-11(human)
|
ELA-11 (human) |
|
|
High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro. |
|
TP2158L |
TRV-120027
|
|
Others
|
|
TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility. |
|
T73690 |
Abaloparatide
|
|
|
|
Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs/cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in... |
|
T68247 |
PSB-KD107
|
|
|
|
PSB-KD107 is an agonist of the Cannabinoid-Activated Orphan G‑Protein-Coupled Receptor GPR18. PSB-KD107 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment... |
|
T76053 |
ELA-11(human) TFA
|
|
|
|
ELA-11(human) TFA, a bioactive fragment of ELA-32, acts as a high-affinity apelin receptor agonist (K i =14 nM). It effectively inhibits forskolin-induced cAMP production and promotes β-arrestin recruitment in vitro, hig... |
|
TP1923 |
Elabela(19-32)
|
ELA-14 (human) |
|
|
Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo. |
|
T79721 |
GPR55 agonist 3
|
|
|
|
Compound 26, a GPR55 agonist, exhibits potent activity with EC50 values of 0.239 nM for hGPR55 and 1.76 nM for rGPR55. It also induces β-arrestin recruitment to human GPR55 with an EC50 of 6.2 nM [1]. |
|
TP2141 |
Balixafortide TFA (1051366-32-5 free base)
|
Balixafortide TFA,POL6326 TFA |
CXCR
|
|
Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-... |
|
T64305 |
APJ receptor agonist 7
|
|
|
|
APJ receptor agonist 7 (compound 37) is an orally active APJ (apelin receptor) agonist (Ki: 0.059 μM). arrestin (EC50: 0.063 μM). |
|
T76044 |
Elabela(19-32) TFA
|
|
|
|
Elabela(19-32) TFA, an effective fragment of ELABELA (ELA), selectively engages with the apelin receptor (APJ). This compound initiates G αi1 and β-arrestin-2 signaling, demonstrating EC50 values of 8.6 nM and 166 nM, re... |
|
T14498 |
Barbadin
|
|
Arrestin
|
|
Barbadin is a novel and specific inhibitor of β-arrestin/β2-adaptin interaction with an IC50 value of 19.1 μM for β-arestin1 and 15.6 μM for β-arestin2. Barbadin potentiates the long term effects of lorcaserin on POMC ne... |
|
TP2141L |
Balixafortide
|
POL6326 |
CXCR
|
|
Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM and it is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects[1]... |
|
T73665 |
Bufrolin
|
|
|
|
Bufrolin, an analog of Cromoglycate (histamine release inhibitor) and a potent agonist of GPR35, enhances the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. It stabilizes mast cells, exhibiting ant... |
|
T36923 |
CXCR2-IN-2
|
CXCR2-IN-2 |
|
|
CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-f... |
|
T75801 |
TC14012 TFA
|
|
|
|
TC14012 TFA, a serum-stable derivative of T140, is a selective peptidomimetic CXCR4 antagonist with an IC50 value of 19.3 nM. It also acts as a potent CXCR7 agonist, exhibiting an EC50 of 350 nM for recruiting β-arrestin... |
|
T69824 |
PSB-17365
|
|
|
|
PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is ... |
|
T69612 |
PSB-KD477
|
|
|
|
PSB-KD477 is an Agonist of the Cannabinoid-Activated Orphan G-Protein-Coupled Receptor GPR18. PSB-KD477 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment... |
|
T75999 |
Balixafortide TFA
|
|
|
|
Balixafortide TFA (POL6326 TFA) is a potent, selective CXCR4 antagonist that exhibits excellent tolerance levels and demonstrates an IC50 of less than 10 nM. It displays over 1000-fold selectivity for CXCR4 over a large ... |
