ligand-binding — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T13884	Shield-1		Others
	Shield-1 is a specific, high-affinity and cell-permeant ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused protein...		Others
T13273	UT-34		Androgen Receptor
	UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prost...		Androgen Receptor
T7904	SR 19881		Estrogen/progestogen Receptor
	SR 19881 is a full agonist of ERRγ(EC50 value of 0.39 μM in a binding assay and an EC50 value of 4.7 μM in a cell-based assay).		Estrogen/progestogen Receptor
T0214	Pioglitazone	U 72107	Ferroptosis , PPAR
	Pioglitazone (U 72107) is an insulin sensitizing agent and thiazolidinedione that is indicated for the treatment of type 2 diabetes. Pioglitazone has been linked to rare instances of acute liver injury.		Ferroptosis , PPAR
T8381	Amodiaquine		Others , Histone Methyltransferase , Parasite
	Amodiaquine is a synthetic aminoquinoline, used to treat malaria.		Others , Histone Methyltransferase , Parasite
T9628	10074-A4		c-Myc
	10074-A4 is a c-Myc binding compound that associates with c-Myc370–409 and behaves like a “ligand cloud” around a “protein cloud”, with distinct features from that of a non-binding ligand.		c-Myc
T11399	Giredestrant	GDC-9545	Estrogen Receptor/ERR , Estrogen/progestogen Receptor
	Giredestrant (GDC-9545) potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain. Giredestrant has anti-tumor activity. Giredestrant, a non-steroidal ER ligand,...		Estrogen Receptor/ERR , Estrogen/progestogen Receptor
T7388	GSK805		ROR
	GSK805 is a potent, orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA bindi...		ROR
T24925	UNC-2170	UNC2170 Maleate,UNC-2170 Maleate,UNC 2170 Maleate	Others
	UNC-2170 (UNC2170 Maleate) is the methyl-lysine binding protein, 53BP1 ligand.		Others
T5160	SR3335	ML 176	ROR
	SR3335 (ML 176) is a selective inverse agonist of RORα, competitively inhibiting the binding of 25-hydroxycholesterol to the ligand binding domain (Ki: 220 nM).		ROR
T13566	Bamirastine	TAK-427	Histamine Receptor
	Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 value of 17.3 nM.Bamirastine has an inhibitory effect on allergic skin inflammation.		Histamine Receptor
T23777	BCI-137	BCI137	Others
	BCI-137 is an Argonaute 2 ligand. It acts by targeting the MicroRNA Binding Domain.		Others
T13848	SMARCA-BD ligand 1 for Protac		Epigenetic Reader Domain
	SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2		Epigenetic Reader Domain
T18787	TD-165		Others , Ligand for E3 Ligase
	TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1].		Others , Ligand for E3 Ligase
T22051	BU 224 hydrochloride		Imidazoline Receptor
	BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.		Imidazoline Receptor
T18595	Dasatinib carbaldehyde	PROTAC ABL binding moiety 4,BMS-354825 carbaldehyde	Others , Ligands for Target Protein for PROTAC
	Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) is based on Dasatinib which is an ABL inhibitor, binds to the IAP ligand via a linker, and forms SNIPER [1].		Others , Ligands for Target Protein for PROTAC
T8486	GW6471	GW 6471	PPAR
	GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.		PPAR
T9108	BI-0115		Lipoxygenase
	BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. It binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX...		Lipoxygenase
T3806	Kaempferide	Kaempferol 4'-O-methyl ether,Kaempferol 4'-methyl ether,4'-Methylkaempferol,4'-O-Methylkaempferol	Estrogen Receptor/ERR , Estrogen/progestogen Receptor , Influenza Virus , Antibacterial , Autophagy
	kaempferide (4'-Methylkaempferol) inhibits the proliferation of native and estrogen receptor beta overexpressing colon cancer cells through a mechanism not mediated by ligand binding dependent estrogen receptor activatio...
T16153	MS4078		ALK , Ligand for E3 Ligase
	MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.		ALK , Ligand for E3 Ligase