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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