Bazedoxifene-Acetate
CAS 198481-33-3
Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.
GPCRs & Receptor Biology
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GPCRs & Receptor Biology products
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LGD2226
CAS 328947-93-9
LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can…
SR59230A
CAS 174689-39-5
SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist[1] with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively[2].
Anamorelin
CAS 249921-19-5
Anamorelin is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
FX-909
CAS 2924573-90-8
FX-909（FX 909） is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that…
AZD5069
CAS 878385-84-3
AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.
Nalfurafine
CAS 152657-84-6
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential[1]. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential…
Rotigotine
CAS 99755-59-6
A non-selective agonist of the dopamine D3 receptor (Ki=0.71 nM); has 10-fold selectivity for the D3 receptor over the D2, D4, and D5 receptors and 100-fold selectivity for the D3 receptor over the D1 receptor; behaves as a full agonist of D1, D2, and D3 with…
Substance P
CAS 33507-63-0
Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Sequence: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.
Aprocitentan (ACT-132577)
CAS 1103522-45-7
ACT-132577 is the major and pharmacologically active metabolite of macitentan, which is dual ETA/ETB antagonist designed for tissue targeting.
Endoxifen
CAS 112093-28-4
Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a…
Aplaviroc HCl
CAS 461023-63-2
Aplaviroc, also known as AK-602; GW-873140; GW873140A; ONO-4128, is a CCR5 entry inhibitor for the potential treatment of HIV infection. Aplaviroc (GW873140) binds specifically to human cellular CC chemokine receptor 5 (CCR5) and demonstrates potent…
Vepdegestrant (ARV-471)
CAS 2229711-68-4
ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.
MIN-101
CAS 359625-79-9
MIN-101 (Roluperidone, CYR-101, MT-210) is a higly potent 5-HT2A and sigma 2 receptor antagonist, with no direct dopamine affinities, for treatment of negative symptoms in schizophrenia. Schizophrenia Phase 3 Clinical
Alfacalcidol
CAS 41294-56-8
Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone…
TTC-352
CAS 1607819-68-0
TTC-352 is a synthetic selective estrogen mimic acts as estrogen receptor (ER) partial agonist for the treatment of endocrine-resistant breast cancer.TTC-352 yields an H-bond with Glu353, allows Asp351-to-helix 12 (H12) interaction, sealing ERα's…
Bremelanotide
CAS 189691-06-3
A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized…
F17464
CAS 1268334-26-4
F17464 is a dopamine D3 receptor preferential antagonist exhibiting high affinity for human dopamine receptor subtype 3 (hD3) (Ki=0.17 nM) and 5-HT1a (Ki=0.16 nM) and a >50 fold lower affinity for the human dopamine receptor subtype 2 short and long form…
ATI-2341
CAS 1337878-62-2
ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
TY-52156
CAS 934369-14-9
TY-52156 is a potent S1P3 receptor antagonist in a competitive manner, and the Ki value is estimated to be 110 nM for S1P3 receptor.
GSK682753A
CAS 1334294-76-6
GSK682753 is a selective and highly potent inverse agonist for murine as well as human EBI2 with inhibition of G protein-dependent signals as well as signals that are probably G protein-independent. In cAMP-response element-binding protein-based reporter and…
LSN3318839
CAS 2764704-18-7
LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).
Cagrilintide
CAS 1415456-99-3
Cagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake.…
Stenabolic (SR9009)
CAS 1379686-30-2
SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
Org 274179-0
CAS 1421683-12-6
Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.
DG-172 dihydrochloride
CAS 1361504-77-9
DG-172 is a novel PPARβ/δ-selective ligand showing high binding affinity (IC50= 27 nM) and potent inverse agonistic properties; inhibits agonist-induced activity of PPARβ/δ, enhances transcriptional corepressor recruitment; down-regulates transcription of the…
J-2156 TFA
CAS 2387505-73-7
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg
GPR30 inhibitor G1
CAS 881639-98-1
A potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM; displays no activity at ERα and ERβ at concentrations up to 10 uM; increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with…
BQ-123
CAS 136553-81-6
BQ-123 is an ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively) . 1) Reduces ischemia-induced ventricular arrhythmias in a rat model.2) BQ-123 prevents LPS-induced preterm birth in mice via the induction…
Difelikefalin (CR845)
CAS 1024828-77-0
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney…
Tabernanthalog
CAS 2483829-58-7
Tabernanthalog is a water-soluble, non-hallucinogenic and non-toxic analogue of ibogaine. Tabernanthalog is a 5-HT2A agonist. Tabernanthalog is found to promote structural neural plasticity, reduce alcohol- and heroin-seeking behaviour, and produce…
SB 265610
CAS 211096-49-0
SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM,…
BX 513 hydrochloride
CAS 1216540-18-9
BX-513 hydrochloride inhibits MIP-1α-induced intracellular calcium mobilization (IC50 = 2.5 μM). Selective CCR1 receptor antagonist (Ki values are 0.04, > 10, > 10 and > 10 nM for CCR1, CCR5, CXCR2 and CXCR4 receptors respectively). A full inverse agonist at…
BMS-986278
CAS 2170126-74-4
BMS-986278 is a potent lysophosphatidic acid receptor 1 (LPA1) antagonist, with a human LPA1 Kb of 6.9 nM.
Mavoglurant (AFQ 056)
CAS 543906-09-8
Mavoglurant is a structurally novel, non-competitive mGlu5 receptor antagonist, has an IC50 of 30 nM in a functional assay with human mGluR5.IC50 value: 30 nMTarget: mGluR5in vitro: Mavoglurant is a selective non-competitive antagonist which showed efficacy…
Fesoterodine fumarate
CAS 286930-03-8
Fesoterodine Fumarate is an antimuscarinic agent and is rapidly de-esterified to its active metabolite 5-hydroxymethyl tolterodine that is a muscarinic receptor antagonist.IC50 value:Target: mAChRFesoterodine has the advantage of allowing more flexible dosage…
Indiplon
CAS 325715-02-4
Potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively). Displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6,…
JD5037
CAS 1392116-14-1
JD-5037 is a novel, peripherally restricted CB1R antagonist with an IC50 of 1.5 nM.
BMS-687453
CAS 1000998-59-3
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
GPR39-C3
CAS 1621175-65-2
TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively.
INCB 8761
CAS 1341224-83-6
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50 of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
XCT790
CAS 725247-18-7
XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.XCT-790 induced cell death in HepG2 hepatocarcinoma and its multi-drug resistance (MDR) sub-line…
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11β-HSD (1)15-PGDH (2)5-HT Receptor (16)Acetyl-CoA Carboxylase (ACC) (3)Acetylcholinesterase (AChE) (2)Ack1 (TNK2) (1)Acyltransferase (1)ADC Cytotoxin (6)ADCs Linker/Click Chemistry (5)Adenosine Receptor (9)Adenylate Cyclase (2)Adrenergic Receptor (11)Akt (12)Alcoholism (2)Aldehyde Dehydrogenase (ALDH) (6)Allergy (5)Alzheimer Disease (13)Aminopeptidase (1)AMPK (8)Amyloids (4)Anaplastic Lymphoma Kinase (ALK) (9)Androgen Receptor (AR) (11)Anemia (4)Angiotensin Receptor (4)Antibody/Protein labeling dyes (1)Antifolate (2)Anxiety (1)Apoptosis Inducer (3)Arginase (1)Arp2/3 complex (1)Aryl hydrocarbon Receptor (AhR) (1)Asthma (5)Atherosclerosis (2)ATM/ATR (8)Aurora Kinase (10)Autophagy (6)Autophagy-related Protein (Atg) (2)Autotaxin (2)Bacterial (26)Bacterial Infection (17)Bcl-2 (14)Bcr-Abl (5)BCRP (1)Beta-catenin (4)Beta-secretase (BACE) (4)Blood Cancer (91)BMI-1 (1)Bone Cancer (6)Brain Cancer (6)Breast Cancer (30)Bromodomain (22)BTK (10)c-Fms (CSF1R) (5)c-Fos/AP-1 (1)c-Kit (6)c-Met (HGFR) 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