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Selectivity data for probe UCSF924 and control UCSF924NC


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UCSF924


Compound concentration: 10 µM
Receptor HGNC target name Inhibition [%] (Primary experimental value) Ki [nM] (Secondary experimental value) pKi
5-HT1B HTR1B 17.68 3408.17 average (n=2) 5.48
Alpha1A ADRA1A 22.97 > 10000.00
Alpha1B ADRA1B 16.51 > 10000.00
Alpha1D ADRA1D 25.43
Alpha2A ADRA2A 17.63 > 10000.00
Alpha2B ADRA2B 21.78 3037.33 average (n=3) 5.59
Alpha2C ADRA2C 44.74 > 10000.00
GABAA/BZP 4.11
D2 DRD2 8.56 4328.00 average (n=2) 5.40
DOR OPRD1 22.46 > 10000.00
M1 CHRM1 12.41 4050.50 average (n=2) 5.40
M2 CHRM2 21.98 4430.00 average (n=3) 5.40
M3 CHRM3 -3.52 > 10000.00
M4 CHRM4 -11.38
M5 CHRM5 15.49
Sigma 1 SIGMAR1 3.82
Sigma 2 TMEM97 50.28 1891.91 5.72
5-HT1A HTR1A 72.14 223.00 average (n=3) 6.67
5-HT1D HTR1D 58.60 3247.50 average (n=4) 5.50
5-HT1E HTR1E -24.77 > 10000.00 average (n=4) < 5.00
5-HT2A HTR2A 19.86 3275.67 average (n=3) 5.50
5-HT2B HTR2B 80.00 236.67 average (n=3) 6.65
5-HT6 HTR6 23.03 6681.00 average (n=2) 5.20
5-HT7A HTR7 60.00 2075.67 average (n=3) 5.68
D1 DRD1 3.15 3415.00 5.50
D3 DRD3 5.75 3193.33 average (n=3) 5.50
D5 DRD5 16.73 > 10000.00 average (n=3) < 5.00
5-HT2C HTR2C 31.68 5550.33 average (n=3) 5.26
5-HT3 HTR3A 54.98 3988.75 average (n=4) 5.43
5-HT5A HTR5A 28.84 5821.50 average (n=2) 5.25
Beta2 ADRB2 33.28 > 10000.00
DAT SLC6A3 52.09 2116.67 average (n=3) 5.79
H1 HRH1 25.54 4553.00 average (n=3) 5.33
H2 HRH2 24.82 1909.67 average (n=3) 5.75
H3 HRH3 -17.18 > 10000.00
NET SLC6A2 26.22
SERT SLC6A4 35.36
D4 DRD4 96.72 4.90 average (n=4) 8.31
H4 HRH4 0.51 > 10000.00
KOR OPRK1 48.39 2307.75 average (n=4) 5.66
MOR OPRM1 39.69 > 10000.00
GABAA 1.68 > 10000.00
GABA/PBR 8.58
Beta1 ADRB1 18.78 > 10000.00
Beta3 ADRB3 11.61
NMDA NMDA 1004.00 6.00
5-HT4 HTR4 6685.00 5.20

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UCSF924

Detailed information about the PRESTO (Parallel Receptor-ome Expression and Screening via Transcriptional Output) -Tango (transcriptional activation following arrestin translocation) GPCR-ome assay can be found here.
Results are expressed in fold of the corresponding basal level. The positive control, DRD2 with 100 nM quinpirole, shows 30x to 100x of basal activity. Generally, the activity ranges from 0.5x to 2.0x fold of basal. Follow-up studies are done when the observed activity is greater than 3.0x fold of basal.

Conclusion: No activity found in panel of 320 non-olfactory GPCRs .

Target protein HGNC name Species Mean fold stimulation SEM
ADCYAP1R1 ADCYAP1R1 Homo sapiens 0.9 0.14
ADORA1 ADORA1 Homo sapiens 1.4 0.03
ADORA2A ADORA2A Homo sapiens 0.5 0.04
ADORA2B ADORA2B Homo sapiens 0.6 0.09
ADORA3 ADORA3 Homo sapiens 0.3 0.00
ADRA1A ADRA1A Homo sapiens 0.3 0.03
ADRA1B ADRA1B Homo sapiens 0.3 0.06
ADRA1D ADRA1D Homo sapiens 0.4 0.04
ADRA2A ADRA2A Homo sapiens 1.6 0.27
ADRA2B ADRA2B Homo sapiens 1.2 0.18
ADRA2C ADRA2C Homo sapiens 1.9 0.50
ADRB1 ADRB1 Homo sapiens 1.1 0.05
ADRB2 ADRB2 Homo sapiens 0.4 0.04
ADRB3 ADRB3 Homo sapiens 1.1 0.24
AGTR1 AGTR1 Homo sapiens 1.1 0.16
AGTR2 AGTR2 Homo sapiens 1.2 0.04
APJ APLNR Homo sapiens 0.8 0.04
AVPR1A AVPR1A Homo sapiens 0.6 0.08
AVPR1B AVPR1B Homo sapiens 0.2 0.03
AVPR2 AVPR2 Homo sapiens 1.6 0.08
BB3 BB3 Homo sapiens 0.8 0.04
BDKBR1 BDKBR1 Homo sapiens 0.6 0.08
BDKBR2 BDKBR2 Homo sapiens 0.3 0.08
C3AR1 C3AR1 Homo sapiens 0.1 0.00
C5A C5AR1 Homo sapiens 0.5 0.10
CALCRb CALCR Homo sapiens 0.5 0.00
CALCRL CALCRL Homo sapiens 1.1 0.24
CASR CASR Homo sapiens 0.4 0.09
CCKAR CCKAR Homo sapiens 0.2 0.03
CCKBR CCKBR Homo sapiens 1.1 0.10
CCR10 CCR10 Homo sapiens 1.0 0.16
CCR2 CCR2 Homo sapiens 0.5 0.03
CCR3 CCR3 Homo sapiens 1.2 0.06
CCR4 CCR4 Homo sapiens 0.3 0.03
CCR5 CCR5 Homo sapiens 0.1 0.03
CCR6 CCR6 Homo sapiens 1.5 0.13
CCR7 CCR7 Homo sapiens 0.3 0.03
CCR8 CCR8 Homo sapiens 1.5 0.33
CCRL2 CCRL2 Homo sapiens 0.5 0.05
CD97 ADGRE5 Homo sapiens 0.7 0.04
CHRM1 CHRM1 Homo sapiens 1.2 0.17
CHRM2 CHRM2 Homo sapiens 0.4 0.05
CHRM3 CHRM3 Homo sapiens 1.5 0.10
CHRM4 CHRM4 Homo sapiens 0.4 0.05
CHRM5 CHRM5 Homo sapiens 0.4 0.04
CMKLR1 CMKLR1 Homo sapiens 0.3 0.03
CNR1 CNR1 Homo sapiens 0.3 0.03
CNR2 CNR2 Homo sapiens 0.4 0.05
CRHR1 CRHR1 Homo sapiens 1.7 0.50
CRHR2 CRHR2 Homo sapiens 0.6 0.06
CX3CR1 CX3CR1 Homo sapiens 0.9 0.18
CXCR1 CXCR1 Homo sapiens 0.5 0.05
CXCR2 CXCR2 Homo sapiens 1.2 0.06
CXCR3 CXCR3 Homo sapiens 1.0 0.03
CXCR4 CXCR4 Homo sapiens 0.7 0.11
CXCR5 CXCR5 Homo sapiens 1.3 0.13
CXCR6 CXCR6 Homo sapiens 0.9 0.13
CXCR7 ACKR3 Homo sapiens 0.6 0.04
CYSLTR1 CYSLTR1 Homo sapiens 0.8 0.09
CYSLTR2 CYSLTR2 Homo sapiens 1.1 0.06
DRD1 DRD1 Homo sapiens 0.2 0.00
DRD2 DRD2 Homo sapiens 0.7 0.06
DRD3 DRD3 Homo sapiens 1.1 0.29
DRD4 DRD4 Homo sapiens 5.3 0.97
DRD5 DRD5 Homo sapiens 0.3 0.05
EDNRA EDNRA Homo sapiens 0.2 0.00
EDNRB EDNRB Homo sapiens 0.7 0.13
ELTD1 ADGRL4 Homo sapiens 1.0 0.17
F2R F2R Homo sapiens 0.5 0.05
F2R-L1 F2RL1 Homo sapiens 0.4 0.04
F2RL2 F2RL2 Homo sapiens 0.5 0.05
F2RL3 F2RL3 Homo sapiens 0.1 0.03
FFA1 FFAR1 Homo sapiens 0.9 0.03
FFA2 FFAR2 Homo sapiens 1.3 0.27
FFA3 FFAR3 Homo sapiens 0.2 0.03
FPR1 FPR1 Homo sapiens 1.6 0.22
FPR2 FPR2 Homo sapiens 0.9 0.12
FPR3 FPR3 Homo sapiens 1.2 0.07
FSHR FSHR Homo sapiens 0.2 0.03
GABBR1 GABBR1 Homo sapiens 0.6 0.05
GAL1 GALR1 Homo sapiens 0.8 0.11
GAL2 GALR2 Homo sapiens 0.6 0.13
GAL3 GALR3 Homo sapiens 0.5 0.03
GCGR GCGR Homo sapiens 0.1 0.03
GHRHR GHRHR Homo sapiens 0.2 0.03
GHSR GHSR Homo sapiens 1.2 0.09
GIPR GIPR Homo sapiens 0.2 0.03
GLP1R GLP1R Homo sapiens 0.2 0.03
GLP2R GLP2R Homo sapiens 0.3 0.03
GMR2 GMR2 Homo sapiens 0.6 0.06
GNRHR GNRHR Homo sapiens 0.2 0.07
GPBA GPBAR1 Homo sapiens 1.4 0.05
GPER GPER1 Homo sapiens 0.3 0.03
GPR1 GPR1 Homo sapiens 0.6 0.09
GPR101 GPR101 Homo sapiens 1.2 0.04
GPR110 ADGRF1 Homo sapiens 0.7 0.07
GPR111 ADGRF2 Homo sapiens 0.4 0.06
GPR113 ADGRF3 Homo sapiens 0.3 0.03
GPR114 ADGRG5 Homo sapiens 0.5 0.03
GPR115 ADGRF4 Homo sapiens 0.6 0.00
GPR116 ADGRF5 Homo sapiens 0.6 0.09
GPR119 GPR119 Homo sapiens 0.9 0.07
GPR12 GPR12 Homo sapiens 1.3 0.08
GPR120 FFAR4 Homo sapiens 1.7 0.73
GPR123 ADGRA1 Homo sapiens 0.4 0.03
GPR124 ADGRA2 Homo sapiens 0.7 0.14
GPR125 ADGRA3 Homo sapiens 0.5 0.03
GPR126 ADGRG6 Homo sapiens 0.7 0.09
GPR132 GPR132 Homo sapiens 0.7 0.10
GPR133 ADGRD1 Homo sapiens 0.4 0.11
GPR135 GPR135 Homo sapiens 0.7 0.12
GPR141 GPR141 Homo sapiens 1.1 0.16
GPR142 GPR142 Homo sapiens 0.2 0.03
GPR143 GPR143 Homo sapiens 0.2 0.03
GPR144 ADGRD2 Homo sapiens 1.0 0.14
GPR146 GPR146 Homo sapiens 0.8 0.13
GPR148 GPR148 Homo sapiens 1.0 0.10
GPR149 GPR149 Homo sapiens 0.6 0.13
GPR15 GPR15 Homo sapiens 0.5 0.14
GPR150 GPR150 Homo sapiens 1.1 0.11
GPR151 GPR151 Homo sapiens 0.2 0.03
GPR152 GPR152 Homo sapiens 0.2 0.03
GPR153 GPR153 Homo sapiens 0.4 0.03
GPR156 GPR156 Homo sapiens 1.3 0.19
GPR157 GPR157 Homo sapiens 0.4 0.04
GPR158 GPR158 Homo sapiens 0.9 0.46
GPR160 GPR160 Homo sapiens 0.9 0.24
GPR161 GPR161 Homo sapiens 0.7 0.08
GPR162 GPR162 Homo sapiens 0.3 0.00
GPR17 GPR17 Homo sapiens 1.4 0.05
GPR171 GPR171 Homo sapiens 1.5 0.46
GPR173 GPR173 Homo sapiens 1.1 0.13
GPR174 GPR174 Homo sapiens 0.6 0.05
GPR176 GPR176 Homo sapiens 0.9 0.17
GPR18 GPR18 Homo sapiens 0.7 0.13
GPR182 GPR182 Homo sapiens 1.1 0.09
GPR183 GPR183 Homo sapiens 0.5 0.05
GPR19 GPR19 Homo sapiens 0.5 0.04
GPR20 GPR20 Homo sapiens 0.9 0.08
GPR21 GPR21 Homo sapiens 0.8 0.08
GPR22 GPR22 Homo sapiens 1.1 0.14
GPR25 GPR25 Homo sapiens 0.7 0.08
GPR26 GPR26 Homo sapiens 0.7 0.05
GPR27 GPR27 Homo sapiens 1.1 0.15
GPR3 GPR3 Homo sapiens 1.3 0.03
GPR31 GPR31 Homo sapiens 0.3 0.03
GPR32 GPR32 Homo sapiens 1.2 0.21
GPR34 GPR34 Homo sapiens 1.5 0.15
GPR35 GPR35 Homo sapiens 0.9 0.08
GPR37 GPR37 Homo sapiens 1.1 0.11
GPR37L1 GPR37L1 Homo sapiens 0.2 0.03
GPR39 GPR39 Homo sapiens 0.3 0.03
GPR4 GPR4 Homo sapiens 0.4 0.03
GPR44 PTGDR2 Homo sapiens 1.5 0.06
GPR45 GPR45 Homo sapiens 0.7 0.17
GPR50 GPR50 Homo sapiens 0.9 0.17
GPR52 GPR52 Homo sapiens 1.1 0.09
GPR55 GPR55 Homo sapiens 0.7 0.10
GPR56 ADGRG1 Homo sapiens 0.9 0.08
GPR6 GPR6 Homo sapiens 1.2 0.08
GPR61 GPR61 Homo sapiens 0.3 0.04
GPR62 GPR62 Homo sapiens 1.1 0.30
GPR63 GPR63 Homo sapiens 0.6 0.09
GPR64 ADGRG2 Homo sapiens 0.9 0.12
GPR65 GPR65 Homo sapiens 0.5 0.00
GPR68 GPR68 Homo sapiens 0.2 0.00
GPR75 GPR75 Homo sapiens 0.9 0.11
GPR77 C5AR2 Homo sapiens 1.2 0.05
GPR78 GPR78 Homo sapiens 1.2 0.13
GPR82 GPR82 Homo sapiens 1.2 0.03
GPR83 GPR83 Homo sapiens 0.2 0.00
GPR84 GPR84 Homo sapiens 1.4 0.27
GPR85 GPR85 Homo sapiens 0.9 0.07
GPR87 GPR87 Homo sapiens 1.1 0.07
GPR88 GPR88 Homo sapiens 2.4 0.13
GPR97 ADGRG3 Homo sapiens 0.3 0.03
GPRC5A GPRC5A Homo sapiens 0.5 0.06
GPRC5B GPRC5B Homo sapiens 0.7 0.06
GPRC5C GPRC5C Homo sapiens 1.3 0.37
GPRC5D GPRC5D Homo sapiens 0.2 0.05
GPRC6A GPRC6A Homo sapiens 0.3 0.07
GRM1 GRM1 Homo sapiens 0.5 0.05
GRM4 GRM4 Homo sapiens 0.3 0.05
GRM5 GRM5 Homo sapiens 0.3 0.04
GRM6 GRM6 Homo sapiens 0.4 0.06
GRM7 GRM7 Homo sapiens 0.3 0.03
GRM8 GRM8 Homo sapiens 0.4 0.03
GRPR GRPR Homo sapiens 0.4 0.12
HCA1 HCAR1 Homo sapiens 0.7 0.10
HCA2 HCAR2 Homo sapiens 0.9 0.09
HCA3 HCAR3 Homo sapiens 0.8 0.18
HCTR1 SLC31A1 Homo sapiens 1.5 0.34
HCTR2 SLC31A2 Homo sapiens 1.1 0.27
HRH1 HRH1 Homo sapiens 1.2 0.08
HRH2 HRH2 Homo sapiens 1.1 0.10
HRH3 HRH3 Homo sapiens 0.9 0.17
HRH4 HRH4 Homo sapiens 1.0 0.06
HTR1A HTR1A Homo sapiens 1.5 0.16
HTR1B HTR1B Homo sapiens 1.2 0.03
HTR1D HTR1D Homo sapiens 1.5 0.04
HTR1E HTR1E Homo sapiens 1.5 0.06
HTR1F HTR1F Homo sapiens 1.3 0.03
HTR2A HTR2A Homo sapiens 0.8 0.05
HTR2B HTR2B Homo sapiens 1.6 0.10
HTR2C INI HTR2C Homo sapiens 1.1 0.35
HTR2C VNV HTR2C Homo sapiens 0.9 0.06
HTR2C VSV HTR2C Homo sapiens 0.5 0.03
HTR2CVGV HTR2C Homo sapiens 0.7 0.05
HTR4 HTR4 Homo sapiens 0.9 0.08
HTR5 HTR5 Homo sapiens 1.1 0.05
HTR6 HTR6 Homo sapiens 1.0 0.13
HTR7 HTR7 Homo sapiens 0.5 0.00
KISSPEPTIN KISS1R Homo sapiens 1.5 0.57
LHCGR LHCGR Homo sapiens 0.6 0.13
LPA4 LPAR4 Homo sapiens 1.1 0.08
LPAR1 LPAR1 Homo sapiens 1.1 0.18
LPAR2 LPAR2 Homo sapiens 1.2 0.34
LPAR5 LPAR5 Homo sapiens 0.7 0.09
LPAR6 LPAR6 Homo sapiens 0.2 0.04
LTB4R LTB4R Homo sapiens 0.8 0.13
LTB4R2B LTB4R2 Homo sapiens 0.3 0.05
MAS1 MAS1 Homo sapiens 0.9 0.06
MAS1L MAS1L Homo sapiens 0.2 0.03
MC1R MC1R Homo sapiens 0.6 0.05
MC2R MC2R Homo sapiens 0.6 0.06
MC3Rb MC3R Homo sapiens 0.4 0.03
MC4R MC4R Homo sapiens 1.0 0.08
MC5R MC5R Homo sapiens 1.0 0.10
MCHR1R MCHR1 Homo sapiens 0.9 0.17
MCHR2R MCHR2 Homo sapiens 0.2 0.03
MLNR MLNR Homo sapiens 0.8 0.17
MRGPRD MRGPRD Homo sapiens 0.9 0.05
MRGPRE MRGPRE Homo sapiens 1.2 0.06
MRGPRF MRGPRF Homo sapiens 0.8 0.05
MRGPRG MRGPRG Homo sapiens 0.2 0.03
MRGPRX1 MRGPRX1 Homo sapiens 0.6 0.06
MRGPRX2 MRGPRX2 Homo sapiens 1.0 0.05
MRGPRX3 MRGPRX3 Homo sapiens 0.9 0.15
MRGPRX4 MRGPRX4 Homo sapiens 1.3 0.06
MTNR1A MTNR1A Homo sapiens 1.5 0.04
MTNR1B MTNR1B Homo sapiens 1.3 0.15
NMBR NMBR Homo sapiens 0.7 0.08
NMUR1 NMUR1 Homo sapiens 0.5 0.06
NMUR2 NMUR2 Homo sapiens 0.3 0.06
NPBW1 NPBWR1 Homo sapiens 0.8 0.03
NPBW2 NPBWR2 Homo sapiens 1.4 0.10
NPFF1 NPFFR1 Homo sapiens 1.0 0.31
NPFF2 NPFFR2 Homo sapiens 1.0 0.22
NPS NPSR1 Homo sapiens 0.6 0.09
NPY1R NPY1R Homo sapiens 0.4 0.06
NPY2R NPY2R Homo sapiens 0.2 0.03
NPY4R NPY4R Homo sapiens 0.4 0.07
NPY5R NPY5R Homo sapiens 0.5 0.03
NTSR1 NTSR1 Homo sapiens 1.0 0.05
NTSR2 NTSR2 Homo sapiens 1.5 0.21
OPN3 OPN3 Homo sapiens 0.8 0.13
OPN5 OPN5 Homo sapiens 1.2 0.04
OPRD1 OPRD1 Homo sapiens 0.7 0.03
OPRK1 OPRK1 Homo sapiens 0.3 0.00
OPRL1 OPRL1 Homo sapiens 0.9 0.17
OPRM1 OPRM1 Homo sapiens 1.0 0.03
OXER1 OXER1 Homo sapiens 0.2 0.03
OXGR1 OXGR1 Homo sapiens 0.9 0.05
OXTR OXTR Homo sapiens 1.0 0.05
P2RY1 P2RY1 Homo sapiens 0.9 0.09
P2RY10 P2RY10 Homo sapiens 0.8 0.03
P2RY11 P2RY11 Homo sapiens 0.4 0.00
P2RY12 P2RY12 Homo sapiens 0.5 0.05
P2RY13 P2RY13 Homo sapiens 1.6 0.16
P2RY14 P2RY14 Homo sapiens 1.1 0.05
P2RY2 P2RY2 Homo sapiens 0.6 0.00
P2RY4 P2RY4 Homo sapiens 0.6 0.03
P2RY6 P2RY6 Homo sapiens 1.3 0.04
P2RY8 P2RY8 Homo sapiens 0.3 0.04
PK1 PROK1 Homo sapiens 0.8 0.06
PK2 PROK2 Homo sapiens 0.7 0.06
PRRP PRLHR Homo sapiens 1.1 0.13
PTAFR PTAFR Homo sapiens 1.2 0.03
PTGDR PTGDR Homo sapiens 1.1 0.10
PTGER1 PTGER1 Homo sapiens 1.3 0.20
PTGER2 PTGER2 Homo sapiens 0.6 0.05
PTGER3 PTGER3 Homo sapiens 0.8 0.10
PTGER4 PTGER4 Homo sapiens 0.4 0.03
PTGFR PTGFR Homo sapiens 0.6 0.03
PTGIR PTGIR Homo sapiens 0.2 0.03
PTH1R PTH1R Homo sapiens 0.5 0.16
PTH2R PTH2R Homo sapiens 0.3 0.00
QRFP QRFP Homo sapiens 0.4 0.07
RXFP1 RXFP1 Homo sapiens 0.3 0.05
RXFP2 RXFP2 Homo sapiens 0.3 0.03
RXFP3 RXFP3 Homo sapiens 0.5 0.03
RXFP4 RXFP4 Homo sapiens 0.5 0.06
S1PR1 S1PR1 Homo sapiens 0.7 0.17
S1PR2 S1PR2 Homo sapiens 1.5 0.21
S1PR3 S1PR3 Homo sapiens 0.8 0.05
S1PR4 S1PR4 Homo sapiens 1.3 0.06
S1PR5 S1PR5 Homo sapiens 1.0 0.05
SCTR SCTR Homo sapiens 1.0 0.06
SSTR1 SSTR1 Homo sapiens 1.0 0.20
SSTR2 SSTR2 Homo sapiens 0.6 0.09
SSTR3 SSTR3 Homo sapiens 0.4 0.05
SSTR4 SSTR4 Homo sapiens 1.8 0.18
SSTR5 SSTR5 Homo sapiens 0.9 0.13
SUCNR1 SUCNR1 Homo sapiens 0.9 0.10
TA1 TAAR1 Homo sapiens 0.5 0.05
TAAR2 TAAR2 Homo sapiens 0.2 0.00
TAAR5 TAAR5 Homo sapiens 0.9 0.22
TAAR6 TAAR6 Homo sapiens 0.3 0.04
TAAR8 TAAR8 Homo sapiens 0.5 0.06
TAAR9 TAAR9 Homo sapiens 0.1 0.00
TACR1 TACR1 Homo sapiens 1.0 0.08
TACR2 TACR2 Homo sapiens 0.7 0.06
TACR3 TACR3 Homo sapiens 0.7 0.10
TBXA2R TBXA2R Homo sapiens 0.1 0.03
TSHR TSHR Homo sapiens 0.2 0.03
UTS2R UTS2R Homo sapiens 1.2 0.11
VIPR1 VIPR1 Homo sapiens 0.6 0.06
VIPR2 VIPR2 Homo sapiens 0.9 0.09