Selectivity data for probe TP-060 and control TP-060n
Coming soon
TP-060
Shown are supplementary data from PMID: 35188773 (S3).
Conclusion: Clean exept for HTR1B HTR1B (EC50 = 2.8 μM), nAChR(a4/b2) Blocker (CHRNA4) (IC50 = 6.5 μM), SLC6A4 (IC50 = 0.31 μM)
| Target protein | HGNC name | Species | Value [µM] | Mode of action |
|---|---|---|---|---|
| ADORA2A | ADORA2A | Homo sapiens | EC50 > 10.0 | Agonist |
| ADORA2A | ADORA2A | Homo sapiens | IC50 > 10.0 | Antagonist |
| ADRA1A | ADRA1A | Homo sapiens | EC50 > 10.0 | Agonist |
| ADRA1A | ADRA1A | Homo sapiens | IC50 > 10.0 | Antagonist |
| ADRA2A | ADRA2A | Homo sapiens | EC50 > 10.0 | Agonist |
| ADRA2A | ADRA2A | Homo sapiens | IC50 > 10.0 | Antagonist |
| ADRB1 | ADRB1 | Homo sapiens | EC50 > 10.0 | Agonist |
| ADRB1 | ADRB1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| ADRB2 | ADRB2 | Homo sapiens | EC50 > 10.0 | Agonist |
| ADRB2 | ADRB2 | Homo sapiens | IC50 > 10.0 | Antagonist |
| AVPR1A | AVPR1A | Homo sapiens | EC50 > 10.0 | Agonist |
| AVPR1A | AVPR1A | Homo sapiens | IC50 > 10.0 | Antagonist |
| CCKAR | CCKAR | Homo sapiens | EC50 > 10.0 | Agonist |
| CCKAR | CCKAR | Homo sapiens | IC50 > 10.0 | Antagonist |
| CHRM1 | CHRM1 | Homo sapiens | EC50 > 10.0 | Agonist |
| CHRM1 | CHRM1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| CHRM2 | CHRM2 | Homo sapiens | EC50 > 10.0 | Agonist |
| CHRM2 | CHRM2 | Homo sapiens | IC50 > 10.0 | Antagonist |
| CHRM3 | CHRM3 | Homo sapiens | EC50 > 10.0 | Agonist |
| CHRM3 | CHRM3 | Homo sapiens | IC50 > 10.0 | Antagonist |
| CNR1 | CNR1 | Homo sapiens | EC50 > 10.0 | Agonist |
| CNR1 | CNR1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| CNR2 | CNR2 | Homo sapiens | EC50 > 10.0 | Agonist |
| CNR2 | CNR2 | Homo sapiens | IC50 > 10.0 | Antagonist |
| DRD1 | DRD1 | Homo sapiens | EC50 > 10.0 | Agonist |
| DRD1 | DRD1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| DRD2S | DRD2 | Homo sapiens | EC50 > 10.0 | Agonist |
| DRD2S | DRD2 | Homo sapiens | IC50 > 10.0 | Antagonist |
| EDNRA | EDNRA | Homo sapiens | EC50 > 10.0 | Agonist |
| EDNRA | EDNRA | Homo sapiens | IC50 > 10.0 | Antagonist |
| HRH1 | HRH1 | Homo sapiens | EC50 > 10.0 | Agonist |
| HRH1 | HRH1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| HRH2 | HRH2 | Homo sapiens | EC50 > 10.0 | Agonist |
| HRH2 | HRH2 | Homo sapiens | IC50 > 10.0 | Antagonist |
| HTR1A | HTR1A | Homo sapiens | EC50 > 10.0 | Agonist |
| HTR1A | HTR1A | Homo sapiens | IC50 > 10.0 | Antagonist |
| HTR1B | HTR1B | Homo sapiens | EC50 = 2.8 | Agonist |
| HTR1B | HTR1B | Homo sapiens | IC50 > 10.0 | Antagonist |
| HTR2A | HTR2A | Homo sapiens | EC50 > 10.0 | Agonist |
| HTR2A | HTR2A | Homo sapiens | IC50 > 10.0 | Antagonist |
| HTR2B | HTR2B | Homo sapiens | EC50 > 10.0 | Agonist |
| HTR2B | HTR2B | Homo sapiens | IC50 > 10.0 | Antagonist |
| OPRD1 | OPRD1 | Homo sapiens | EC50 > 10.0 | Agonist |
| OPRD1 | OPRD1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| OPRK1 | OPRK1 | Homo sapiens | EC50 > 10.0 | Agonist |
| OPRK1 | OPRK1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| OPRM1 | OPRM1 | Homo sapiens | EC50 > 10.0 | Agonist |
| OPRM1 | OPRM1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| CAV1.2 | CACNA1C | Rattus sp. | IC50 > 10.0 | Blocker |
| GABAA | Rattus sp. | IC50 > 10.0 | Blocker | |
| GABAA | Rattus sp. | EC50 > 10.0 | Opener | |
| hERG | KCNH2 | Homo sapiens | IC50 > 10.0 | Blocker |
| HTR3A | HTR3A | Homo sapiens | IC50 > 10.0 | Blocker |
| HTR3A | HTR3A | Homo sapiens | EC50 > 10.0 | Opener |
| KvLQT1/minK |
KCNQ1 KCNE1 |
Homo sapiens | IC50 > 10.0 | Blocker |
| KvLQT1/minK |
KCNQ1 KCNE1 |
Homo sapiens | EC50 > 10.0 | Opener |
| nAChR(a4/b2) | CHRNA4 | Homo sapiens | IC50 = 6.5 | Blocker |
| nAChR(a4/b2) | CHRNA4 | Homo sapiens | EC50 > 10.0 | Opener |
| NAV1.5 | SCN5A | Homo sapiens | IC50 > 10.0 | Blocker |
| NMDAR(1A/2B) | Rattus sp. | IC50 > 10.0 | Blocker | |
| NMDAR(1A/2B) | Rattus sp. | EC50 > 10.0 | Opener | |
| INSR | INSR | Homo sapiens | IC50 > 10.0 | Inhibitor |
| LCK | LCK | Homo sapiens | IC50 > 10.0 | Inhibitor |
| ROCK1 | ROCK1 | Homo sapiens | IC50 > 10.0 | Inhibitor |
| VEGFR2 | KDR | Homo sapiens | IC50 > 10.0 | Inhibitor |
| AR | AR | Homo sapiens | EC50 > 10.0 | Agonist |
| AR | AR | Homo sapiens | IC50 > 10.0 | Antagonist |
| GR | NR3C1 | Homo sapiens | EC50 > 10.0 | Agonist |
| GR | NR3C1 | Homo sapiens | IC50 > 10.0 | Antagonist |
| AChE | ACHE | Homo sapiens | IC50 > 10.0 | Inhibitor |
| COX1 | COX1 | Homo sapiens | IC50 > 10.0 | Inhibitor |
| COX2 | COX2 | Homo sapiens | IC50 > 10.0 | Inhibitor |
| MAOA | MAOA | Rattus sp. | IC50 > 10.0 | Inhibitor |
| PDE3A | PDE3A | Homo spaiens | IC50 > 10.0 | Inhibitor |
| PDE4D2 | PDE4D2 | Homo spaiens | IC50 > 10.0 | Inhibitor |
| DAT | SLC6A3 | Homo sapiens | IC50 > 10.0 | Blocker |
| NET | SLC6A2 | Homo sapiens | IC50 > 10.0 | Blocker |
| SERT | SLC6A4 | Homo sapiens | IC50 = 0.3 | Blocker |