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Potency data for probe JP3000 and control JP3001


In vitro potency


Target name Target information Species Assay description Probe result (SD) Control result (SD) Publication of assay conditions
RXRA RXRA ligand binding domain Homo sapiens ITC (RXRA) Kd < 10 nM

In cell potency


Target name Target information Species Assay description Probe result (SD) Control result (SD) Publication of assay conditions
RXRA hinge region and LBD Homo sapiens Hybrid reporter gene assay (RXRA): These test systems rely on a chimera receptor containing only the ligand binding domain of the nuclear receptor in which is fused to the DNA binding domain from the yeast receptor Gal4. HEK293T cells EC50 = 5 nM ± 1.000 nM (n=3) EC50 > 10 µM (n=3)
RXRB hinge region and LBD Homo sapiens Hybrid reporter gene assay (RXRB): These test systems rely on a chimera receptor containing only the ligand binding domain of the nuclear receptor in which is fused to the DNA binding domain from the yeast receptor Gal4. HEK293T cells EC50 = 1.400 nM ± 0.400 nM (n=3) EC50 > 10 µM (n=3)
RXRG hinge region and LBD Homo sapiens Hybrid reporter gene assay (RXRG): These test systems rely on a chimera receptor containing only the ligand binding domain of the nuclear receptor in which is fused to the DNA binding domain from the yeast receptor Gal4. HEK293T cells EC50 = 4 nM ± 1.000 nM (n=3) EC50 > 10 µM (n=3)
RXRA, RXRB, RXRG full length Homo sapiens Full-length RXR reporter gene assay (RXR:RXR Homodimer): transiently transfected HEK293T cells using firefly lucifease reporter constructs EC50 = 2.600 nM ± 0.300 nM (n=3)
RXRA, RXRB, RXRG, RARA, RARB Homo sapiens Full-length RXR reporter gene assay (RXR;RAR Heterodimer): transiently transfected HEK293T cells using firefly lucifease reporter constructs EC50 = 29 nM ± 2.000 nM (n=3)
RXRA, RXRB, RXRG HT-29 cells Homo sapiens GDE1 expression: induction of RXR-regulated gene expression/ qRT-PCR/GDE1 mRNA expression was normalized to GAPDH mRNA expression per each sample using the ΔCt-method. EC50 ~ 10 nM