Compound ID | Pharmacological profile | Compound name | Binding data | Activity data | Bibliographic ref | Cross-reactivity | |
CHEMBL1801746 | agonist | Compound 10 | PMID: 21561094 | ||||
CHEMBL1801747 | agonist | Compound 11 | PMID: 21561094 | ||||
CHEMBL1807060 | agonist | Compound 8 | PMID: 21618996 | ||||
CHEMBL1807061 | agonist | Compound 3 | PMID: 21561094 | ||||
CHEMBL1807063 | agonist | Compound 9 | PMID: 21618996 | ||||
CHEMBL238908 | agonist | Compound ent-2 | PMID: 17963371 | ||||
CHEMBL240597 | agonist | Compound 2 | PMID: 17963371 | FXR_alpha | |||
CHEMBL242293 | agonist | Compound 10 | pIC50 = 7.2 | pEC50 = 7.8 | PMID: 17215127 | ||
CHEMBL242526 | agonist | Compound 2 | pIC50 = 5.0 | pEC50 = 6.0 | PMID: 17215127 | ||
CHEMBL242527 | agonist | Compound 3 | pIC50 = 5.4 | pEC50 = 6.3 | PMID: 17215127 | ||
CHEMBL242528 | agonist | Compound 5 | pIC50 = 6.5 | pEC50 = 6.8 | PMID: 17215127 | ||
CHEMBL259223 | agonist | Compound 6 | PMID: 21561094 | ||||
CHEMBL261696 | agonist | Compound 5 | PMID: 21561094 | ||||
CHEMBL263382 | agonist | vitamin K2 | PMID: 12920130 | ||||
CHEMBL370872 | antagonist | UCL2158H | IC50 = 14.61 µM / max % inhibition = 109 | PMID: 18583127 | |||
CHEMBL374478 | agonist | rifampicin | EC50 = 710 µM | PMID: 10748001 | |||
CHEMBL388024 | agonist | Compound 4 | pIC50 = 6.6 | pEC50 = 6.9 | PMID: 17215127 | ||
CHEMBL392740 | agonist | Compound ent-1 | PMID: 17963371 | ||||
CHEMBL396952 | agonist | Compound 9 | pIC50 = 7.6 | pEC50 = 8.5 | PMID: 17215127 | ||
CHEMBL396953 | agonist | Compound 11 | pIC50 = 6.2 | pEC50 = 6.0 | PMID: 17215127 | ||
CHEMBL430006 | agonist | Compound 12 | pIC50 = 7.7 | pEC50 = 8.0 | PMID: 17215127 | ||
CHEMBL450449 | antagonist | Ecteinascidin-743 | IC50 = 3nM | PMID: 11329060 | |||
CHEMBL457271 | agonist | C2BA-4 (1) | EC50 = 49 +/- 15 nM | PMID: 18304819 | |||
CID8273 | antagonist | bromocresol purple | PMID: 20869355 | ||||
ZINC00001219 | antagonist | coumestrol | IC50 = 12 µM | PMID: 18096694 | ER_alpha | ||
ZINC00004785 | agonist | carbamazepine | EC50 = 15.6 +/- 7.64 µM | PMID: 16328606 | |||
ZINC00056964 | antagonist | bisphenol S | PMID: 20869355 | ||||
ZINC00599734 | agonist | lansoprazole | EC50 = 3.02 +/- 1.95 µM | PMID: 16328606 | |||
ZINC00601283 | agonist | indomethacin | EC50 = 17.6 +/- 7.90 µM | PMID: 16328606 | |||
ZINC00968279 | agonist | troglitazone | EC50 = 3.45 +/- 0.84 µM | PMID: 16328606 | PPAR_gamma | ||
ZINC01530862 | agonist | primaquine | EC50 = 13.6 +/- 6.10 µM | PMID: 16328606 | |||
ZINC01537619 | agonist | Compound 1 | pEC50 = 6.6 | PMID: 21907579 | |||
ZINC01550221 | agonist | T0901317 | pIC50 = 7.4 | pEC50 = 7.9 | PMID: 17215127 | LXR_alpha | |
ZINC01751810 | agonist | TCPOBOP | EC50 = 3.9 µM | PMID: 10748001 | CAR | ||
ZINC02000967 | agonist | schisandrin A | EC50 = 1.25 µM | PMID: 16267138 | |||
ZINC02169963 | agonist | lithocholic acid | Ki = 9 µM | PMID: 11248085 | |||
ZINC02510358 | agonist | phenytoin | EC50 = 8.03 +/- 5.18 µM | PMID: 16328606 | |||
ZINC03137566 | agonist | phenobarbital | EC50 = 370 +/- 11 µM | PMID: 15548381 | |||
ZINC03633644 | agonist | Compound 3 | pEC50 = 7.8 | PMID: 21907579 | |||
ZINC03799969 | agonist | SR12813 | Ki = 41 nM | EC50 = 120 n M | PMID: 10748001 | ||
ZINC03807804 | agonist | clotrimazole | EC50 = 1.6 µM | PMID: 10748001 | CAR | ||
ZINC03831128 | agonist | mifepristone | EC50 = 5.5 µM | PMID: 10748001 |
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ZINC03860920 | antagonist | thymolphtalein | PMID: 20869355 | ||||
ZINC03871832 | agonist | verapamil | EC50 = 3.19 +/- 1.42 µM | PMID: 16328606 | |||
ZINC03875332 | agonist | dexamethasone | EC50 = 5-10 µM | PMID: 9727070 | |||
ZINC03875544 | agonist | warfarin | EC50 = 49.5 +/- 16 µM | PMID: 16328606 | |||
ZINC03876136 | agonist | betamethasone | EC50 = 19.9 +/- 1.59 µM | PMID: 16328606 | |||
ZINC04098025 | agonist | artemisin | EC50 = 5-34 µM | PMID: 15761118 | |||
ZINC04676424 | agonist | pantoprazole | EC50 = 6.84 +/- 2.16 µM | PMID: 16328606 | |||
ZINC04693574 | agonist | omeprazole | EC50 = 8.63 +/- 3.14 µM | PMID: 16328606 | |||
ZINC06036225 | agonist | 3-keto-litocholic acid | Ki = 15 µM | PMID: 11248085 | VDR | ||
ZINC06718468 | agonist | Compound 1 | %transactivation = 90-123 | PMID: 20153189 | |||
ZINC07992661 | agonist | (+)-S20 | EC50 = 400 nM | PMID: 15872116 | |||
ZINC12496506 | agonist | rabeprazole | EC50 = 1.49 +/- 0.58 µM | PMID: 16328606 | |||
ZINC14514081 | agonist | hyperforin | Ki = 27 nM | EC50 = 23 nM | PMID: 10852961 | ||
ZINC19594578 | agonist | nifedipine | Fold induction = 10 | PMID: 9770465 | MR | ||
ZINC29040943 | agonist | Compound 2a | %transactivation = 147 | PMID: 20153189 | |||
ZINC29044661 | agonist | Compound 2 | EC50 = 1.6 µM | PMID: 21334894 | |||
ZINC29128555 | agonist | Compound 8a | activation = 89 % | PMID: 18240388 | |||
ZINC29128965 | agonist | Compound 7a | activation = 99 % | PMID: 18240388 | |||
ZINC29129212 | agonist | Compound 6c | activation = 95 % | PMID: 18240388 | |||
ZINC38558781 | agonist | Compound 4 | EC50 = 1.7 µM | PMID: 21334894 | |||
ZINC40379700 | agonist | Compound 6c | EC50 = 23 +/- 10 nM | PMID: 18304819 | |||
ZINC40380137 | agonist | Compound 6g | EC50 = 336 +/- 217 nM | PMID: 18304819 | |||
ZINC40380280 | agonist | Compound 9a | EC50 = 1456 +/- 746 nM | PMID: 18304819 | |||
ZINC40380552 | agonist | Compound 15b | EC50 = 55 +/ -19 nM | PMID: 18304819 | |||
ZINC40392094 | agonist | Compound 10a | EC50 = 515 +/- 281 nM | PMID: 18304819 | |||
ZINC40392398 | agonist | Compound 6k | EC50 = 45 +/- 13 nM | PMID: 18304819 | |||
ZINC40392807 | agonist | Compound 6e | EC50 = 101 +/- 33 nM | PMID: 18304819 | |||
ZINC40392984 | agonist | Compound 6o | EC50 = 42 +/- 10 nM | PMID: 18304819 | |||
ZINC40393413 | agonist | Compound 6j | EC50 = 388 +/- 105 nM | PMID: 18304819 | |||
ZINC40393539 | agonist | Compound 6p | EC50 = 52 +/- 12 nM | PMID: 18304819 | |||
ZINC40431134 | agonist | Compound 38 | EC50 = 2.4 µM | PMID: 18440811 | |||
ZINC40846385 | agonist | Compound 8 | EC50 = 197 +/- 200 nM | PMID: 18304819 | |||
ZINC40846401 | agonist | Compound 15a | EC50 = 385 +/- 239 nM | PMID: 18304819 | |||
ZINC40848165 | agonist | Compound 6h | EC50 = 20 +/- 9 nM | PMID: 18304819 | |||
ZINC40848293 | agonist | Compound 6a | EC50 = 176 +/- 73 nM | PMID: 18304819 | |||
ZINC40848294 | agonist | Compound 6b | EC50 = 428 +/- 104 nM | PMID: 18304819 | |||
ZINC40848457 | agonist | Compound 6f | EC50 = 271 +/- 98 nM | PMID: 18304819 | |||
ZINC40848459 | agonist | Compound 6i | EC50 = 51 +/- 16 nM | PMID: 18304819 | |||
ZINC40860415 | agonist | Compound 7a | EC50 = 376 +/- 230 nM | PMID: 18304819 | |||
ZINC40860417 | agonist | Compound 7b | EC50 = 340 +/- 110 nM | PMID: 18304819 | |||
ZINC40866727 | agonist | Compound 6l | EC50 = 33 +/- 11 nM | PMID: 18304819 | |||
ZINC40866754 | agonist | Compound 14a | EC50 = 55 +/- 32 nM | PMID: 18304819 | |||
ZINC40867190 | agonist | Compound 6m | EC50 = 1.5 +/- 0.5 nM | PMID: 18304819 | |||
ZINC40872710 | agonist | Compound 6n | EC50 = 0.7 +/- 0.3 nM | PMID: 18304819 | |||
ZINC40873157 | agonist | Compound 10b | EC50 = 217 +/- 144 nM | PMID: 18304819 | |||
ZINC40873818 | agonist | Compound 6d | EC50 = 20 +/- 8 nM | PMID: 18304819 | |||
ZINC40878501 | agonist | Compound 14b | EC50 = 13 +/ - 5 nM | PMID: 18304819 | |||
ZINC40936229 | antagonist | FL-B-12 | IC50 = 13.68 µM ; max % inhibition = 103 | PMID: 18583127 | |||
ZINC40953929 | agonist | Compound 35 | EC50 = 1.7 µM | PMID: 18440811 | |||
ZINC49016487 | agonist | Compound 4c | %transactivation = 120 | PMID: 20153189 | |||
ZINC49020143 | agonist | Compound 4d | %transactivation = 113 | PMID: 20153189 | |||
ZINC49872045 | agonist | Compound 4l | %transactivation = 102 | PMID: 20153189 | |||
ZINC51119024 | agonist | Compound 1 | EC50 = 1.1 µM | PMID: 18763755 | |||
ZINC66099714 | agonist | solomonsterol A | EC50 = 5.2 +/- 0.4 µM | PMID: 21599020 | |||
ZINC66112511 | agonist | Compound 2 | PMID: 21141967 | ||||
ZINC71281670 | agonist | theonellesterol F | PMID: 21428459 | ||||
ZINC71281761 | agonist | theonellesterol C | PMID: 21428459 | FXR_alpha | |||
ZINC71282148 | agonist | theonellesterol E | PMID: 21428459 | FXR_alpha | |||
ZINC71294190 | agonist | Conicasterol D | PMID: 21428459 | FXR_alpha | |||
ZINC71294251 | agonist | Conicasterol B | PMID: 21428459 | FXR_alpha | |||
ZINC71294416 | agonist | theonellesterol H | PMID: 21428459 | ||||
ZINC71294448 | agonist | theonellesterol D | PMID: 21428459 | FXR_alpha | |||
ZINC71295100 | agonist | theonellesterol G | PMID: 21428459 | ||||
ZINC71295392 | agonist | theonellesterol B | PMID: 21428459 | FXR_alpha | |||
ZINC73385923 | agonist | conicasterol E | PMID: 22126372 | FXR_alpha |