Selectivity data for probe GSK778
Jump to control PDSP data
GSK778
Compound concentration: 10 µM| Receptor | HGNC target name | Inhibition [%] (Primary experimental value) | Ki [nM] (Secondary experimental value) | pKi |
|---|---|---|---|---|
| Beta1 | ADRB1 | 4.82 | ||
| Beta3 | ADRB3 | 10.53 | ||
| GABAA/BZP | 91.62 | 1970.29 average (n=2) | 5.75 | |
| GABAA | 52.72 | 1595.89 average (n=2) | 5.81 | |
| GABA/PBR | 7.75 | |||
| D4 | DRD4 | 79.54 | 856.99 average (n=2) | 6.09 |
| D5 | DRD5 | 31.66 | ||
| DAT | SLC6A3 | 27.90 | ||
| H4 | HRH4 | 29.26 | ||
| KOR | OPRK1 | 15.54 | ||
| MOR | OPRM1 | 16.87 | ||
| NET | SLC6A2 | 34.50 | ||
| Alpha1A | ADRA1A | 0.31 | ||
| Alpha1B | ADRA1B | 4.20 | ||
| Alpha1D | ADRA1D | 17.03 | ||
| Alpha2A | ADRA2A | 9.95 | ||
| Alpha2B | ADRA2B | -13.60 | ||
| Alpha2C | ADRA2C | 15.35 | ||
| M1 | CHRM1 | -1.37 | ||
| M2 | CHRM2 | 4.05 | ||
| M3 | CHRM3 | -3.35 | ||
| Sigma 2 | TMEM97 | 23.02 | ||
| 5-HT1A | HTR1A | 15.28 | ||
| 5-HT1B | HTR1B | 8.66 | ||
| 5-HT1D | HTR1D | 14.83 | ||
| 5-HT1E | HTR1E | -19.46 | ||
| 5-HT2A | HTR2A | -5.06 | ||
| 5-HT2B | HTR2B | -10.48 | ||
| 5-HT6 | HTR6 | -9.08 | ||
| 5-HT7A | HTR7 | -5.39 | ||
| D1 | DRD1 | 2.89 | ||
| D2 | DRD2 | 27.74 | ||
| D3 | DRD3 | 62.41 | 485.92 average (n=2) | 6.39 |
| 5-HT2C | HTR2C | -0.02 | ||
| 5-HT3 | HTR3A | 69.83 | 4456.49 average (n=2) | 5.35 |
| 5-HT5A | HTR5A | 21.48 | ||
| Beta2 | ADRB2 | 18.37 | ||
| DOR | OPRD1 | 38.45 | ||
| H1 | HRH1 | 0.33 | ||
| H2 | HRH2 | 12.29 | ||
| H3 | HRH3 | -5.03 | ||
| M4 | CHRM4 | 15.71 | ||
| M5 | CHRM5 | 24.55 | ||
| SERT | SLC6A4 | 10.71 | ||
| Sigma 1 | SIGMAR1 | 38.49 |
GSK778
A panel of bromodomain containing proteins (BCP) was screened in a dose-response format in duplicate.
Conclusion: Clean panel. GSK778 displayed selective binding within the BET family and over 100-fold selectivity for BRD4 BD1 over BRD4 BD2.
| Target protein | HGNC name | Species | Kd [nM] |
|---|---|---|---|
| ATAD2A | ATAD2 | Homo sapiens | > 30000.0 |
| ATAD2B | ATAD2B | Homo sapiens | 25000.0 |
| BAZ2A | BAZ2A | Homo sapiens | > 30000.0 |
| BAZ2B | BAZ2B | Homo sapiens | > 30000.0 |
| BRD1 | BRD1 | Homo sapiens | > 30000.0 |
| BRD2(1) | BRD2 | Homo sapiens | 13.0 |
| BRD2(2) | BRD2 | Homo sapiens | 840.0 |
| BRD3(1) | BRD3 | Homo sapiens | 5.0 |
| BRD3(2) | BRD3 | Homo sapiens | 310.0 |
| BRD4(1) | BRD4 | Homo sapiens | 5.9 |
| BRD4(1,2) | BRD4 | Homo sapiens | 100.0 |
| BRD4(2) | BRD4 | Homo sapiens | 670.0 |
| BRD4(FULL-LENGTH,SHORT-ISO.) | BRD4 | Homo sapiens | 11.0 |
| BRD7 | BRD7 | Homo sapiens | > 30000.0 |
| BRD9 | BRD9 | Homo sapiens | > 30000.0 |
| BRDT(1) | BRDT | Homo sapiens | 18.0 |
| BRDT(2) | BRDT | Homo sapiens | 5400.0 |
| BRPF1 | BRPF1 | Homo sapiens | 15000.0 |
| BRPF3 | BRPF3 | Homo sapiens | > 30000.0 |
| CECR2 | CECR2 | Homo sapiens | > 30000.0 |
| CREBBP | CREBBP | Homo sapiens | 3800.0 |
| EP300 | EP300 | Homo sapiens | 5700.0 |
| FALZ | BPTF | Homo sapiens | > 30000.0 |
| GCN5L2 | KAT2A | Homo sapiens | > 30000.0 |
| PBRM1(2) | PBRM1 | Homo sapiens | 29000.0 |
| PBRM1(5) | PBRM1 | Homo sapiens | > 30000.0 |
| PCAF | KAT2B | Homo sapiens | 33000.0 |
| SMARCA2 | SMARCA2 | Homo sapiens | > 30000.0 |
| TAF1(2) | TAF1 | Homo sapiens | > 30000.0 |
| TAF1L(2) | TAF1L | Homo sapiens | > 30000.0 |
| TRIM24(BROMO.) | TRIM24 | Homo sapiens | > 30000.0 |
| TRIM24(PHD,Bromo.) | TRIM24 | Homo sapiens | > 30000.0 |
| TRIM33(PHD,Bromo.) | TRIM33 | Homo sapiens | > 30000.0 |
| WDR9(2) | BRWD1 | Homo sapiens | > 30000.0 |
GSK778
Shown are supplementary data from PMID: 32787145.
Conclusion: Clean panel
| Target protein | HGNC name | Species | Value | Mode of action | Assay | Source |
|---|---|---|---|---|---|---|
| 5-HT Transporter (SERT) | SLC6A4 | Homo sapiens | pIC50 = 4.4 | Binding | SPA | BacMam |
| 5-HT1B | HTR1B | Homo sapiens | pEC50 < 4.0 | Agonist | 10 µL GTPγS LEADseeker | |
| 5-HT1B | HTR1B | Homo sapiens | pIC50 < 4.0 | Antagonist | 10 µL GTPγS LEADseeker | |
| 5-HT2A | HTR2A | Homo sapiens | pEC50 < 4.6 | Agonist | Luminescence | HEK |
| 5-HT2A | HTR2A | Homo sapiens | pIC50 < 4.6 | Antagonist | Luminescence | HEK |
| 5-HT2C | HTR2C | Homo sapiens | pEC50 < 4.6 | Agonist | Luminescence | CHO |
| 5-HT2C | HTR2C | Homo sapiens | pIC50 < 4.6 | Antagonist | Luminescence | CHO |
| 5HT3 | HTR3A | Homo sapiens | pEC50 < 4.3 | Agonist | FLIPR | |
| Acetylcholinesterase (AChE) | ACHE | Homo sapiens | pIC50 = 4.2 | RapidFire Mass Spec | ||
| Adenosine A2a | ADORA2A | Homo sapiens | pEC50 < 4.0 | Agonist | LANCE TR-FRET | Whole cell |
| Adrenergic Alpha 1B | ADRA1B | Homo sapiens | pIC50 < 4.6 | Antagonist | Intracell Ca | |
| Alpha 1 nAChR | CHRNA1 | Homo sapiens | pEC50 < 4.3 | Agonist | FLIPR | HEK293 |
| Alpha 1 nAChR | CHRNA1 | Homo sapiens | pIC50 = 6.0 | Antagonist | FLIPR | HEK293 |
| Alpha 2C Adrenoceptor | ADRA2C | Homo sapiens | pEC50 < 4.0 | LANCE TR-FRET | CHO-K1 | |
| Aurora B/INCENP | AURKB | Homo sapiens | pIC50 < 4.5 | 30 min IMAP 2 µM ATP | ||
| Beta2 Adrenoceptor | ADRB2 | Homo sapiens | pEC50 < 4.0 | Agonist | TR-FRET | |
| Beta2 Adrenoceptor | ADRB2 | Homo sapiens | pIC50 < 4.0 | Antagonist | TR-FRET | |
| Cannabinoid CB2 Receptor | CNR2 | Homo sapiens | pEC50 < 4.0 | Agonist | FDGlu | Yeast |
| Cyclooxygenase 2 (COX-2) | PTGS2 | Homo sapiens | pIC50 < 4.0 | FLINT | ||
| Cytochrome P450 3A4 | CYP3A4 | Homo sapiens | pIC50 = 5.2 | Vivid Green FLINT | ||
| Cytochrome P450 3A4 | CYP3A4 | Homo sapiens | pIC50 = 6.0 | Vivid Red FLINT | ||
| Dopamine 2 (D2) | DRD2 | Homo sapiens | pIC50 = 5.5 | Antagonist | GTPγS SPA | |
| Dopamine D1 | DRD1 | Homo sapiens | pIC50 < 4.0 | Antagonist | LANCE TR-FRET | |
| Dopamine D2 | DRD2 | Homo sapiens | pEC50 < 4.0 | Agonist | Low Na GTPγS SPA | HEK293F |
| Histamine Receptor H1 (HRH1) | HRH1 | Homo sapiens | pIC50 < 4.6 | Antagonist | Luminescence | |
| 5HT3 | HTR3A | Homo sapiens | pIC50 < 4.3 | Antagonist | FLIPR | |
| CaV1.2 (L-type) Calcium Channel | CACNA1C | Homo sapiens | pIC50 < 4.0 | Barracuda Ephys | ||
| Monoamine Oxidase (MAO) B Inhibitor | MAOB | Homo sapiens | pIC50 = 4.1 | FLINT | ||
| KCNH2 (hERG) | KCNH2 | Homo sapiens | pIC50 = 4.4 | Antagonist | Barracuda Ephys PPC | |
| KCNQ1/KCNE1 (Kv7.1/MinK) |
KCNQ1 KCNE1 |
Homo sapiens | pIC50 < 4.6 | Blocker | Electrophys | CHO |
| Kv1.5 (KCNA5) | KCNA5 | Homo sapiens | pIC50 < 4.3 | Blocker | Electrophys | CHO |
| LCK | LCK | Homo sapiens | pIC50 < 4.5 | IMAP | ||
| M1 (CHRM1) | CHRM1 | Homo sapiens | pEC50 < 4.3 | Agonist | Intracellular Ca Fluorescence | CHO |
| M1 (CHRM1) | CHRM1 | Homo sapiens | pIC50 < 4.3 | Antagonist | Intracellular Ca Fluorescence | CHO |
| M2 (CHRM2) | CHRM2 | Homo sapiens | pEC50 < 4.3 | Agonist | Intracellular Ca Fluorescence | CHO |
| M2 (CHRM2) | CHRM2 | Homo sapiens | pIC50 = 5.0 | Antagonist | Intracellular Ca Fluorescence | CHO |
| NaV1.5 | SCN5A | Homo sapiens | pIC50 = 4.3 | Blocker | IonWorks Electrophys 2 Hz | HEK |
| NK1 | TACR1 | Homo sapiens | pIC50 < 4.6 | Antagonist | Aequorin Luminescence | U2OS |
| Noradrenaline Transporter (NET) | SLC6A2 | Homo sapiens | pIC50 = 4.7 | Binding | SPA | BacMam |
| NR2B (NR1A/2B) Subunit | GRIN2B | Homo sapiens | pIC50 < 4.3 | Antagonist | FLIPR | U2OS |
| OPRK1 | OPRK1 | Homo sapiens | pEC50 < 4.0 | Agonist | GTPγS LEADseeker | BacMam |
| OPRK1 | OPRK1 | Homo sapiens | pIC50 < 4.0 | Antagonist | GTPγS LEADseeker | BacMam |
| OPRM1 | OPRM1 | Homo sapiens | pEC50 < 4.0 | Agonist | GTPγS LEADseeker | BacMam |
| Organic Anion Transport Polypeptide C OATP1B1 | SLCO1B1 | pIC50 = 4.4 | Image | HEK | ||
| PDE4B | PDE4B | Homo sapiens | pIC50 = 4.4 | Luminescence | ||
| Phosphodiesterase 3A (PDE3A) | PDE3A | pIC50 < 4.0 | Inhibition | [3H]-cAMP SPA | [3H]-cAMP | |
| Phospholipidosis induction | pMEC < 4.0 | FLINT Fluorescence | HepG2 | |||
| PI3K-gamma | PIK3CG | Homo sapiens | pIC50 < 4.5 | Inhibition | TR-FRET | |
| PXR (NR1I2) | NR1I2 | Homo sapiens | pEC50 < 4.3 | Agonist | FuGENE 25 µL | HepG2 |
| Vasopressin V1a | AVPR1A | Homo sapiens | pIC50 < 4.3 | Antagonist | Double wash FLIPR |