Selectivity data for probe BAY-9835 and control BAY-1880
Coming soon
BAY-9835
BAY-9835 was used at 10 µM.
Conclusion: Clean panel.
| Target protein | HGNC name | Species | Cmp. conc. | % Inhibition | Assay ID |
|---|---|---|---|---|---|
| Cholinesterase, Acetyl, ACES | ACHE | Homo sapiens | 10 µM | 3.0 | 104010 |
| Aldose Reductase | AKR1B1 | Rattus sp. | 10 µM | -4.0 | 107000 |
| Peptidase, Angiotensin Converting Enzyme | ACE | Oryctolagus cuniculus | 10 µM | 3.0 | 107300 |
| ATPase, Na+/K+, Heart, Pig | Sus scrofa | 10 µM | -5.0 | 107710 | |
| Carbonic Anhydrase II | CA2 | Homo sapiens | 10 µM | -2.0 | 112020 |
| Cyclooxygenase COX-1 | PTGS1 | Homo sapiens | 10 µM | -5.0 | 116020 |
| Cyclooxygenase COX-2 | PTGS2 | Homo sapiens | 10 µM | 11.0 | 118010 |
| HMG-CoA Reductase | HMGCR | Homo sapiens | 10 µM | -5.0 | 124010 |
| Leukotriene LTC4 Synthase | LTC4S | Cavia porcellus | 10 µM | -14.0 | 132000 |
| Monoamine Oxidase MAO-A | MAOA | Homo sapiens | 10 µM | 0.0 | 140010 |
| Monoamine Oxidase MAO-B | MAOB | Homo sapiens | 10 µM | 10.0 | 140120 |
| Nitric Oxide Synthase, Neuronal (nNOS) | NOS1 | Rattus sp. | 10 µM | 0.0 | 142000 |
| Phosphodiesterase PDE3 | Homo sapiens | 10 µM | 11.0 | 152000 | |
| Phosphodiesterase PDE4D2 | PDE4D | Homo sapiens | 10 µM | 3.0 | 154420 |
| Phosphodiesterase PDE5 | PDE5A | Homo sapiens | 10 µM | -5.0 | 156000 |
| Thromboxane Synthase | TBXAS1 | Homo sapiens | 10 µM | 11.0 | 194020 |
| Nitric Oxide Synthetase, Inducible (iNOS) | NOS2 | Mus musculus | 10 µM | 0.0 | 199010 |
| Lipoxygenase 15-LO | ALOX15 | Homo sapiens | 10 µM | -6.0 | 199017 |
| Adenosine A1 | ADORA1 | Homo sapiens | 10 µM | -4.0 | 200510 |
| Adenosine A2A | ADORA2A | Homo sapiens | 10 µM | 3.0 | 200610 |
| Adenosine A3 | ADORA3 | Homo sapiens | 10 µM | 0.0 | 200720 |
| Transporter, Adenosine | Homo sapiens | 10 µM | 11.0 | 202020 | |
| Adrenergic alpha1A | ADRA1A | Rattus sp. | 10 µM | -14.0 | 203100 |
| Adrenergic alpha2A | ADRA2A | Homo sapiens | 10 µM | -3.0 | 203630 |
| Adrenergic alpha2B | ADRA2B | Homo sapiens | 10 µM | -3.0 | 203710 |
| Adrenergic alpha2C | ADRA2C | Homo sapiens | 10 µM | -1.0 | 203810 |
| Adrenergic beta1 | ADRB1 | Homo sapiens | 10 µM | -8.0 | 204010 |
| Adrenergic beta2 | ADRB2 | Homo sapiens | 10 µM | -9.0 | 204110 |
| Adrenergic beta3 | ADRB3 | Homo sapiens | 10 µM | -3.0 | 204200 |
| Transporter, Norepinephrine (NET) | SLC6A2 | Homo sapiens | 10 µM | 6.0 | 204410 |
| Androgen (Testosterone) | AR | Homo sapiens | 10 µM | 3.0 | 206000 |
| Angiotensin AT1 | AGTR1 | Homo sapiens | 10 µM | -1.0 | 210030 |
| Angiotensin AT2 | AGTR2 | Homo sapiens | 10 µM | 0.0 | 210120 |
| Bradykinin B1 | BDKRB1 | Homo sapiens | 10 µM | 1.0 | 212520 |
| Bradykinin B2 | BDKRB2 | Homo sapiens | 10 µM | -6.0 | 212620 |
| Cannabinoid CB1 | CNR1 | Homo sapiens | 10 µM | -3.0 | 217030 |
| Cannabinoid CB2 | CNR2 | Homo sapiens | 10 µM | -1.0 | 217100 |
| Dopamine D1 | DRD1 | Homo sapiens | 10 µM | -1.0 | 219500 |
| Dopamine D2L | DRD2 | Homo sapiens | 10 µM | 2.0 | 219600 |
| Dopamine D2S | DRD2 | Homo sapiens | 10 µM | 0.0 | 219700 |
| Dopamine D3 | DRD3 | Homo sapiens | 10 µM | 2.0 | 219800 |
| Transporter, Dopamine (DAT) | SLC6A3 | Homo sapiens | 10 µM | 7.0 | 220320 |
| Endothelin ETA | EDNRA | Homo sapiens | 10 µM | 2.0 | 224010 |
| Endothelin ETB | EDNRB | Homo sapiens | 10 µM | -17.0 | 224110 |
| Estrogen ERalpha | ESR1 | Homo sapiens | 10 µM | 13.0 | 226010 |
| Transporter, GABA | Rattus sp. | 10 µM | 7.0 | 226400 | |
| GABAA, Flunitrazepam, Central | Rattus sp. | 10 µM | -6.0 | 226600 | |
| GABAA, Chloride Channel, TBOB | Rattus sp. | 10 µM | 0.0 | 226810 | |
| GABAB, Non-Selective | GABBR1 | Rattus sp. | 10 µM | 3.0 | 228510 |
| Glucocorticoid | NR3C1 | Homo sapiens | 10 µM | 3.0 | 232030 |
| Glutamate, AMPA | Rattus sp. | 10 µM | -11.0 | 232600 | |
| Glutamate, Kainate | Rattus sp. | 10 µM | 12.0 | 232710 | |
| Glutamate, NMDA, Agonism | Rattus sp. | 10 µM | 1.0 | 232810 | |
| Glutamate, NMDA, Glycine | Rattus sp. | 10 µM | -4.0 | 232910 | |
| Growth Hormone Secretagogue (GHS, Ghrelin) | GHSR | Homo sapiens | 10 µM | 6.0 | 239300 |
| Histamine H1 | HRH1 | Homo sapiens | 10 µM | -1.0 | 239610 |
| Histamine H2 | HRH2 | Homo sapiens | 10 µM | 16.0 | 239710 |
| Histamine H3 | HRH3 | Homo sapiens | 10 µM | 6.0 | 239820 |
| Insulin | INSR | Rattus sp. | 10 µM | -8.0 | 243000 |
| Motilin | MLNR | Homo sapiens | 10 µM | 3.0 | 252200 |
| Muscarinic M1 | CHRM1 | Homo sapiens | 10 µM | -6.0 | 252610 |
| Muscarinic M2 | CHRM2 | Homo sapiens | 10 µM | 1.0 | 252710 |
| Muscarinic M3 | CHRM3 | Homo sapiens | 10 µM | 9.0 | 252810 |
| Muscarinic M4 | CHRM4 | Homo sapiens | 10 µM | -6.0 | 252910 |
| Nicotinic Acetylcholine alpha3beta4 |
CHRNA3 CHRNB4 |
Homo sapiens | 10 µM | 2.0 | 258730 |
| Opiate delta1 (OP1, DOP) | OPRD1 | Homo sapiens | 10 µM | 18.0 | 260130 |
| Opiate kappa (OP2, KOP) | OPRK1 | Homo sapiens | 10 µM | -4.0 | 260210 |
| Opiate mu (OP3, MOP) | OPRM1 | Homo sapiens | 10 µM | 2.0 | 260410 |
| Purinergic P2Y | Rattus sp. | 10 µM | -4.0 | 268810 | |
| Serotonin (5-Hydroxytryptamine) 5-HT1A | HTR1A | Homo sapiens | 10 µM | -3.0 | 271110 |
| Serotonin (5-Hydroxytryptamine) 5-HT2A | HTR2A | Homo sapiens | 10 µM | -7.0 | 271650 |
| Serotonin (5-Hydroxytryptamine) 5-HT2B | HTR2B | Homo sapiens | 10 µM | -1.0 | 271700 |
| Serotonin (5-Hydroxytryptamine) 5-HT2C | HTR2C | Homo sapiens | 10 µM | -1.0 | 271800 |
| Transporter, Serotonin (5-Hydroxytryptamine) (SERT) | SLC6A4 | Homo sapiens | 10 µM | 10.0 | 274030 |
| Vasopressin V1A | AVPR1A | Homo sapiens | 10 µM | 7.0 | 287530 |
| Progesterone PR-B | PGR | Homo sapiens | 10 µM | -13.0 | 299005 |
| Purinergic P2X | Rattus sp. | 10 µM | 0.0 | 299036 |
BAY-9835
Assay description can be found on slide 12 in ' BAY-9835 Inhibitor for ADAMTS7 and ADAMTS12.pdf' or in the supplements of PMID: 38348661.
Conclusion: The protease panel is clean.
| Target protein | HGNC name | Species | IC50 [µM] |
|---|---|---|---|
| hADAMTS4 | ADAMTS4 | Homo sapiens | 6.7 |
| hADAMTS5 | ADAMTS5 | Homo sapiens | 9.9 |
| hADAM8 | ADAM8 | Homo sapiens | 2.3 |
| hADAM10 | ADAM10 | Homo sapiens | 32.8 |
| hADAM17 | ADAM17 | Homo sapiens | 5.8 |
| hMMP2 | MMP2 | Homo sapiens | > 100.0 |
| hMMP12 | MMP12 | Homo sapiens | 5.4 |
| hMMP14 | MMP14 | Homo sapiens | > 100.0 |
| hMMP15 | MMP15 | Homo sapiens | 78.5 |
| Calpain 1 | CAPN1 | Homo sapiens | > 100.0 |
| Caspase 3 | CASP3 | Homo sapiens | > 100.0 |
| Cathepsin B | CTSB | Homo sapiens | > 100.0 |
| Cathepsin S | CTSS | Homo sapiens | > 100.0 |
| MALT1 | MALT1 | Homo sapiens | > 100.0 |