Selectivity data for probe JNJ-8003 and control JNJ-6643
Coming soon
JNJ-8003
Closest off-target is TSPO (BBR) (IC50 = 0.56 µM).
Conclusion: Change date
| Target protein | HGNC name | Species | Cmp. conc. | % Inhibition | IC50 [µM] | Ki [µM] | Reference compound name | Reference compound IC50 [nM] | Assay ID |
|---|---|---|---|---|---|---|---|---|---|
| GAL1 | GALR1 | Homo sapiens | 10 µM | < 10.0 | galanine porcine | 0.11 | Cerep_62 | ||
| A3 | ADORA3 | Homo sapiens | 10 µM | 46.3 | 49.00 | IB-MECA | 0.37 | Cerep_6 | |
| alpha 1 (non-selective) |
ADRA1A ADRA1B ADRA1D |
Rattus norvegicus | 10 µM | 25.6 | prazosin | 0.26 | Cerep_8 | ||
| PBR | TSPO | Homo sapiens | 10 µM | 54.1 | 0.56 | 0.51 | PK 11195 | 1.30 | Cerep_3643 |
| CB1 | CNR1 | Homo sapiens | 10 µM | 23.3 | CP 55940 | 1.00 | Cerep_4708 | ||
| D5 | DRD5 | Homo sapiens | 10 µM | 11.0 | SCH 23390 | 0.59 | Cerep_50 | ||
| TNF-alpha | TNFRSF1A | Homo sapiens | 10 µM | 17.8 | TNF-alpha | 0.09 | Cerep_76 | ||
| MT1 (ML1A) | MTNR1A | Homo sapiens | 10 µM | 29.0 | melatonin | 0.21 | Cerep_1538 | ||
| NK1 | TACR1 | Homo sapiens | 10 µM | 45.4 | 8.40 | [Sar9,Met(O2)11]-SP | 0.42 | Cerep_100 | |
| NK2 | TACR2 | Homo sapiens | 10 µM | 52.7 | 6.80 | [Nleu10]-NKA (4-10) | 1.80 | Cerep_102 | |
| NK3 | TACR3 | Homo sapiens | 10 µM | 21.7 | SB 222200 | 5.30 | Cerep_104 | ||
| Y2 | NPY2R | Homo sapiens | 10 µM | 11.4 | NPY | 0.21 | Cerep_107 | ||
| delta (DOP) | OPRD1 | Homo sapiens | 10 µM | 25.8 | DPDPE | 2.10 | Cerep_114 | ||
| kappa (KOP) | OPRK1 | Homo sapiens | 10 µM | 28.5 | U50488 | 0.70 | Cerep_4461 | ||
| NOP (ORL1) | OPRL1 | Homo sapiens | 10 µM | 10.8 | nociceptin | 0.10 | Cerep_358 | ||
| PPARgamma | PPARG | Homo sapiens | 10 µM | 35.8 | rosiglitazone | 12.00 | Cerep_641 | ||
| EP2 | PTGER2 | Homo sapiens | 10 µM | 23.1 | PGE2 | 5.20 | Cerep_1955 | ||
| EP4 | PTGER4 | Homo sapiens | 10 µM | 75.9 | 1.30 | PGE2 | 0.79 | Cerep_441 | |
| 5-HT2B | HTR2B | Homo sapiens | 10 µM | 23.7 | (±)DOI | 3.40 | Cerep_1333 | ||
| 5-HT2C | HTR2C | Homo sapiens | 10 µM | 31.3 | RS 102221 | 4.80 | Cerep_137 | ||
| 5-HT5a | HTR5A | Homo sapiens | 10 µM | 19.8 | serotonin | 260.00 | Cerep_140 | ||
| 5-HT6 | HTR6 | Homo sapiens | 10 µM | 12.7 | serotonin | 220.00 | Cerep_142 | ||
| GR | NR3C1 | Homo sapiens | 10 µM | 35.8 | dexamethasone | 1.80 | Cerep_469 | ||
| V1a | AVPR1A | Homo sapiens | 10 µM | 10.6 | [d(CH2)51,Tyr(Me)2]-AVP | 2.60 | Cerep_159 | ||
| Cl-channel (GABA-gated) | Rattus norvegicus | 10 µM | 57.6 | 7.40 | 6.10 | picrotoxinin | 220.00 | Old_Cerep_16 | |
| dopamine transporter | SLC6A3 | Homo sapiens | 10 µM | 36.5 | BTCP | 9.80 | Cerep_52 | ||
| A1 | ADORA1 | Homo sapiens | 10 µM | < 10.0 | DPCPX | 1.30 | Cerep_2 | ||
| A2A | ADORA2A | Homo sapiens | 10 µM | < 10.0 | NECA | 58.00 | Cerep_4 | ||
| alpha 2 (non-selective) |
ADRA2A ADRA2B ADRA2C |
Rattus norvegicus | 10 µM | < 10.0 | yohimbine | 110.00 | Cerep_11 | ||
| beta 1 | ADRB1 | Homo sapiens | 10 µM | < 10.0 | atenolol | 250.00 | Cerep_18 | ||
| beta 2 | ADRB2 | Homo sapiens | 10 µM | < 10.0 | ICI 118551 | 0.75 | Cerep_20 | ||
| AT1 | AGTR1 | Homo sapiens | 10 µM | < 10.0 | saralasin | 1.00 | Cerep_24 | ||
| AT2 | AGTR2 | Homo sapiens | 10 µM | < 10.0 | angiotensin-II | 0.12 | Cerep_26 | ||
| BZD (central) | Rattus norvegicus | 10 µM | < 10.0 | diazepam | 8.90 | Old_Cerep_37 | |||
| BB (non-selective) | Rattus norvegicus | 10 µM | < 10.0 | bombesin | 0.54 | Cerep_30 | |||
| B2 | BDKRB2 | Homo sapiens | 10 µM | < 10.0 | NPC 567 | 25.00 | Cerep_33 | ||
| CGRP | CALCRL | Homo sapiens | 10 µM | < 10.0 | hCGRPalpha | 0.03 | Cerep_373 | ||
| CCK1 (CCKA) | CCKAR | Homo sapiens | 10 µM | < 10.0 | CCK-8s | 0.16 | Cerep_39 | ||
| CCK2 (CCKB) | CCKBR | Homo sapiens | 10 µM | < 10.0 | CCK-8s | 0.16 | Cerep_41 | ||
| D1 | DRD1 | Homo sapiens | 10 µM | < 10.0 | SCH 23390 | 0.74 | Cerep_44 | ||
| D2S | DRD2 | Homo sapiens | 10 µM | < 10.0 | (+)butaclamol | 3.50 | Old_Cerep_1322 | ||
| D3 | DRD3 | Homo sapiens | 10 µM | < 10.0 | (+)butaclamol | 3.00 | Cerep_48 | ||
| D4.4 | DRD4 | Homo sapiens | 10 µM | < 10.0 | clozapine | 73.00 | Cerep_49 | ||
| ETA | EDNRA | Homo sapiens | 10 µM | < 10.0 | endothelin-1 | 0.08 | Cerep_54 | ||
| ETB | EDNRB | Homo sapiens | 10 µM | < 10.0 | endothelin-3 | 0.02 | Cerep_56 | ||
| GABA (non-selective) | Rattus norvegicus | 10 µM | < 10.0 | GABA | 38.00 | Cerep_57 | |||
| GAL2 | GALR2 | Homo sapiens | 10 µM | < 10.0 | galanin | 0.37 | Cerep_410 | ||
| PDGF | Mus musculus | 10 µM | < 10.0 | PDGF BB | 0.25 | Cerep_70 | |||
| CXCR2 (IL-8B) | CXCR2 | Homo sapiens | 10 µM | < 10.0 | IL-8 | 0.33 | Cerep_419 | ||
| CCR1 | CCR1 | Homo sapiens | 10 µM | < 10.0 | MIP-1alpha | 0.04 | Cerep_361 | ||
| H1 | HRH1 | Homo sapiens | 10 µM | < 10.0 | pyrilamine | 1.80 | Cerep_870 | ||
| H2 | HRH2 | Homo sapiens | 10 µM | < 10.0 | cimetidine | 700.00 | Cerep_1208 | ||
| MC4 | MC4R | Homo sapiens | 10 µM | < 10.0 | NDP-alpha -MSH | 0.46 | Cerep_420 | ||
| M1 | CHRM1 | Homo sapiens | 10 µM | < 10.0 | pirenzepine | 33.00 | Cerep_91 | ||
| M2 | CHRM2 | Homo sapiens | 10 µM | < 10.0 | methoctramine | 51.00 | Cerep_93 | ||
| M3 | CHRM3 | Homo sapiens | 10 µM | < 10.0 | 4-DAMP | 1.90 | Cerep_95 | ||
| M4 | CHRM4 | Homo sapiens | 10 µM | < 10.0 | 4-DAMP | 1.10 | Cerep_96 | ||
| M5 | CHRM5 | Homo sapiens | 10 µM | < 10.0 | 4-DAMP | 1.30 | Cerep_97 | ||
| Y1 | NPY1R | Homo sapiens | 10 µM | < 10.0 | NPY | 0.09 | Cerep_106 | ||
| NTS1 (NT1) | NTSR1 | Homo sapiens | 10 µM | < 10.0 | neurotensin | 0.31 | Cerep_109 | ||
| mu (MOP) | OPRM1 | Homo sapiens | 10 µM | < 10.0 | DAMGO | 0.95 | Cerep_118 | ||
| PAC1 (PACAP) | ADCYAP1R1 | Homo sapiens | 10 µM | < 10.0 | PACAP1-38 | 0.08 | Cerep_1518 | ||
| PCP | Rattus norvegicus | 10 µM | < 10.0 | MK 801 | 17.00 | Old_Cerep_32 | |||
| IP (PGI2) | PTGIR | Homo sapiens | 10 µM | < 10.0 | iloprost | 13.00 | Cerep_2230 | ||
| P2X | Rattus norvegicus | 10 µM | < 10.0 | alpha, beta - MeATP | 2.70 | Old_Cerep_127 | |||
| P2Y | Rattus norvegicus | 10 µM | < 10.0 | dATPalpha S | 91.00 | Cerep_128 | |||
| 5-HT1A | HTR1A | Homo sapiens | 10 µM | < 10.0 | 8-OH-DPAT | 1.20 | Cerep_131 | ||
| 5-HT1B | HTR1B | Homo sapiens | 10 µM | < 10.0 | Serotonine | 210.00 | Cerep_4376 | ||
| 5-HT2A | HTR2A | Homo sapiens | 10 µM | < 10.0 | ketanserin | 1.00 | Cerep_135 | ||
| 5-HT3 | HTR3A | Homo sapiens | 10 µM | < 10.0 | MDL 72222 | 11.00 | Cerep_411 | ||
| 5-HT7 | HTR7 | Homo sapiens | 10 µM | < 10.0 | serotonin | 0.63 | Cerep_144 | ||
| sigma (non-selective) | Homo sapiens | 10 µM | < 10.0 | haloperidol | 140.00 | Cerep_3500 | |||
| sst (non-selective) | Mus musculus | 10 µM | < 10.0 | somatostatin-14 | 0.17 | Cerep_149 | |||
| VPAC1 (VIP1) | VIPR1 | Homo sapiens | 10 µM | < 10.0 | VIP | 0.52 | Cerep_157 | ||
| Ca2+ channel (L,verapamil site) (phenylalkylamine) | Rattus norvegicus | 10 µM | < 10.0 | D 600 | 39.00 | Cerep_163 | |||
| KV channel | Rattus norvegicus | 10 µM | < 10.0 | alpha- dendrotoxin | 0.14 | Cerep_166 | |||
| SKCa channel | Rattus norvegicus | 10 µM | < 10.0 | apamin | 0.03 | Cerep_167 | |||
| Na+ channel (site2) | Rattus norvegicus | 10 µM | < 10.0 | veratridine | 8400.00 | Old_Cerep_169 | |||
| norepinephrine transporter | SLC6A2 | Homo sapiens | 10 µM | < 10.0 | protriptyline | 5.00 | Cerep_355 | ||
| 5-HT transporter | SCL6A4 | Homo sapiens | 10 µM | < 10.0 | imipramine | 3.00 | Cerep_439 |