Table 2.
Activity expressed as percentage inhibition of 10 μM BIRB0796 on 76 GPCRs within Millipore’s Safety and Liability Panel.
| GPCR | Percentage inhibition |
|---|---|
| 5-HT1A | 31.0 |
| 5-HT2A | 99.5 |
| 5-HT2B | 18.5 |
| 5-HT2C | 5.5 |
| A1 | 19.5 |
| A3 | 20.5 |
| Alpha1A | 6.0 |
| Alpha1D | 3.5 |
| Alpha2A | −4.0 |
| AT1 | −2.5 |
| B2 | −4.5 |
| BB2 | 0.0 |
| Beta 1 | −6.0 |
| Beta 2 | −9.5 |
| BLT1 | 8.5 |
| C5aR | −5.5 |
| CB1 | 9.0 |
| CB2 | 80.0 |
| CCK2 | 2.0 |
| CCR1 | −6.0 |
| CCR2B | 0.0 |
| CGRP1 | 0.0 |
| CRF1 | 13.0 |
| CX3CR1 | −12.0 |
| CXCR1 | −1.5 |
| CysLT1 | 2.0 |
| D1 | 23.0 |
| D2L | 53.5 |
| D5 | 14.0 |
| DP | 12.5 |
| EP2 | 2.5 |
| EP3 | 7.5 |
| ETA | −4.0 |
| ETB | 11.0 |
| FP | 20.5 |
| FPR1 | −4.5 |
| GAL1 | −1.5 |
| GnRH/LHRH | −20.5 |
| GPR109A | −1.0 |
| H1 | −1.5 |
| H2 | −5.5 |
| H3 | 91.5 |
| IP1 | 12.5 |
| LPA1 | 6.5 |
| LPA3 | 5.0 |
| M1 | 46.5 |
| M2 | 34.5 |
| M3 | 5.0 |
| MC5 | 2.0 |
| Motilin receptor | 94.5 |
| NK1 | 12.0 |
| NK3 | 17.5 |
| NMU1 | 22.5 |
| NTR1 | −12.0 |
| OPRD1 | 8.5 |
| OPRK1 | −19.0 |
| OPRM1 | −2.5 |
| OT | 12.5 |
| OX1 | 12.0 |
| P2Y1 | 10.5 |
| PAC1 long isoform | 3.5 |
| PAF | 19.5 |
| PK1 | −6.5 |
| PRP | 3.0 |
| PTH1 | 0.0 |
| S1P3 | −1.5 |
| SST4 | −5.5 |
| TP | 32.0 |
| Trypsin-mediated PARs | 9.0 |
| TSH | −4.0 |
| UT/GPR14 | 18.5 |
| V1A | 2.0 |
| V2 | 1.0 |
| VPAC1 | −2.0 |
| VPAC2 | −4.0 |
| Y2 | −13.5 |
Red font is used to highlight the targets where the inhibition observed was >50%. All GPCRs within Millipore’s Safety and Liability Panel are full length human isoforms.