Potency data for probe SAFit2 and controls ddSAFit2, 18(S)-Me
In vitro potency
| Target name | Target information | Species | Assay description | SAFit2 | ddSAFit2, 18(S)-Me | Publication of assay conditions |
|---|---|---|---|---|---|---|
| FKBP5 | FK506-binding domain of FKBP51 (4.5 nM) | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP5): 3 nM of iFit-FL was used as a tracer. | Kd = 6 nM ± 2.000 nM | Kd > 20 µM | PMID: 25436518 |
| FKBP1B | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP1B): 3 nM of iFit-FL was used as a tracer. | Kd = 38.9 nM ± 3.000 nM | PMID: 25436518 | ||
| FKBP1A | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP1A): 3 nM of iFit-FL was used as a tracer. | Kd = 116.4 nM ± 7.100 nM | PMID: 25436518 | ||
| FKBP2 | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP2): 3 nM of iFit-FL was used as a tracer. | Kd = 1053 nM ± 93.000 nM | PMID: 25436518 | ||
| FKBP3 | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP3): 3 nM of iFit-FL was used as a tracer. | Kd > 10 µM | PMID: 25436518 | ||
| FKBP4 | Homo sapiens | Competitive fluorescence polarization binding assay (FKBP4): 3 nM of iFit-FL was used as a tracer. | Kd > 50 µM | PMID: 25436518 |
In cell potency
| Target name | Target information | Species | Assay description | SAFit2 | ddSAFit2, 18(S)-Me | Publication of assay conditions |
|---|---|---|---|---|---|---|
| FKBP5 | HEK293Tcells stably over-expressing FKBP12-NLuc | Homo sapiens | NanoBRET assay (FKBP12-NLuc): 20 nM of tracer 2b | IC50 = 195.5 nM ± 14.000 nM | PMID: 33887102 | |
| FKBP5 | HEK293Tcells stably over-expressing FKBP51-NLuc | Homo sapiens | NanoBRET assay (FKBP51-NLuc) (FKBP5): 200 nM of tracer 2c | IC50 = 493 nM ± 101.000 nM | PMID: 33887102 | |
| FKBP1A | HEK293Tcells stably over-expressing FKBP51-NLuc | Homo sapiens | NanoBRET assay (FKBP51-NLuc) (FKBP1A): 200 nM of tracer 2c | IC50 = 1103 nM ± 86.000 nM | PMID: 33887102 | |
| FKBP1A | HEK293Tcells stably over-expressing FKBP12-NLuc | Homo sapiens | NanoBRET assay (FKBP12-NLuc) (FKBP1A): 20 nM of tracer 2b | IC50 = 771 nM ± 115.000 nM | PMID: 33887102 | |
| FKBP1B | HEK293Tcells stably over-expressing FKBP12-NLuc | Homo sapiens | NanoBRET assay (FKBP12-NLuc) (FKBP1B): 20 nM of tracer 2b | IC50 = 80 nM ± 21.000 nM | PMID: 33887102 | |
| FKBP4 | HEK293Tcells stably over-expressing FKBP12-NLuc | Homo sapiens | NanoBRET assay (FKBP12-NLuc) (FKBP4): 20 nM of tracer 2b | IC50 = 1409 nM ± 92.000 nM | PMID: 33887102 |