Potency data for probe JNJ-8003 and control JNJ-6643
In vitro potency
| Target name | Target information | Species | Assay description | Compound conc. | JNJ-8003 | JNJ-6643 | Publication of assay conditions |
|---|---|---|---|---|---|---|---|
| RSV L, RSV P | purified RSV L + P complex | Human respiratory syncytial virus | Thermal shift assay (RSV L + P complex) | 25 µM | deltaTm = 6 °C | PMID: 37865687 (supplement) | |
| RSV L, RSV P | Purified recombinant RSV L+P complex (C-terminal 6x His-tag on the P protein) | Human respiratory syncytial virus | Surface plasmon resonance (RSV L + P complex): on-rate = 2.16 μM−1 s−1, slow off-rate = 0.0000181 s−1 | Kd = 0.84 nM | PMID: 37865687 (supplement) | ||
| RSV L, RSV P, RSV P | Recombinant RSV L+P complex | Human respiratory syncytial virus | Biotinylated primer extension Flashplate enzymatic assay: Inhibition of RNA synthesis activity | IC50 = 0.67 nM (n=4) | IC50 = 530 nM (n=1) | PMID: 39105710 | |
| RSV L, RSV P | RSV-L + P complex (expressed from insect cells) | Human respiratory syncytial virus | SPA primer extensions enzymatic assay | IC50 = 0.29 nM | PMID: 39105710 | ||
| RSV L, RSV P | Recombinant RSV L+P complex | Human respiratory syncytial virus | RSV L+P primer extension assay testing RNA-dependent RNA polymerase activity | IC50 = 0.73 nM (n=18) | PMID: 37865687 | ||
| POLA1 | Homo sapiens | DNA-dependant DNA polymerase activity assay (POLA1): DNA polymerase alpha (CHIMERx) | IC50 > 100 µM | PMID: 37865687 (supplement) | |||
| POLB | Homo sapiens | DNA-dependant DNA polymerase activity assay (POLB): DNA polymerase beta (CHIMERx) | IC50 > 100 µM | PMID: 37865687 (supplement) | |||
| POLG | Homo sapiens | DNA-dependant DNA polymerase activity assay (POLG): DNA polymerase gamma (Abcam) | IC50 > 100 µM | PMID: 37865687 (supplement) | |||
| POLRMT | Homo sapiens | Mitochondrial RNA polymerase-DdRp activity | IC50 > 100 µM | PMID: 37865687 (supplement) | |||
| POLR2L | Homo sapiens | RNA polymerase II-DdRp activity | IC50 > 100 µM | PMID: 37865687 (supplement) |
In cell potency
| Target name | Target information | Species | Assay description | JNJ-8003 | JNJ-6643 | Publication of assay conditions |
|---|---|---|---|---|---|---|
| RSV L, RSV P, RSV P | HeLa cells | Human respiratory syncytial virus | RSV cell-based infection assay (eGFP assay) in HeLa cells: RSV-A2-eGFP (rgRSV224) | EC50 = 0.82 nM | EC50 = 150 nM | PMID: 37865687 |
| RSV L, RSV P | APC-126 cells | Human respiratory syncytial virus | RSV sub-genomic replicon assay (APC-126 cells) | EC50 = 0.15 nM (n=24) | PMID: 39105710 | |
| RSV L, RSV P | HeLa cells | Human respiratory syncytial virus | HeLa cell based reporter assay: Inhibition against RSV A2 replication using rgRSV224 reporter strain | EC50 = 0.78 nM (n=23) | PMID: 37865687 | |
| RSV L, RSV P | HeLa cells | Human respiratory syncytial virus | RT-qPCR (HeLa cells) for RSV A: median of 10 strains (clinical isolates and laboratory strains) | EC50 = 0.18 nM (n=10) | PMID: 37865687 | |
| RSV L, RSV P | HeLa cells | Human respiratory syncytial virus | RT-qPCR (HeLa cells) for RSV B: median of 6 strains (clinical isolates and laboratory strains) | EC50 = 0.1 nM (n=6) | PMID: 37865687 | |
| LLC-MK2 cells | Human metapneumovirus CAN97-83 | Reporter assay (HMPV) | EC50 = 0.88 µM | PMID: 37865687 (supplement) | ||
| LLC-MK2 cells | Human Parainfluenza Virus Type 1 Washington/20993/1964 | Reporter assay (PIV-1) | EC50 = 13 µM | PMID: 37865687 (supplement) | ||
| LLC-MK2 cells | Human Parainfluenza Virus Type 3 JS | Reporter assay (PIV-3) | EC50 = 11 µM | PMID: 37865687 (supplement) | ||
| A549 cells | Vesicular stomatitis virus Indiana | Reporter assay (VSV) | EC50 > 25 µM | PMID: 37865687 (supplement) |