TABLE 2.
Range of Reported Ki and Kd Values (µM) | ||||||||
---|---|---|---|---|---|---|---|---|
Ligand | FABP1 | FABP2 | FABP3 | FABP4 | FABP5 | FABP7 | ||
Acifluorfen | 4.2-8.9 | |||||||
ANS | 1.1-6.0 1.1a | 12b | 3.0-31c | 0.6 | 0.03-32 | 0.07-1.3 | ||
Aspirin | 348a | 3780b | 300-460 | |||||
Atenolol | 717 | NBc | ||||||
Benzafibrate | NBa | 44.4b | 26-100c | NB | 12 | NB | ||
Benzilic acid | 110.8-200c | |||||||
Benzyl salicylate | NB | |||||||
Bifenox | NB | |||||||
BMS309403 | 0.9 | |||||||
CBD | 4.0 | 1.7 | 1.9 | 1.5 | ||||
Ciprofibrate | 24-72c | |||||||
Clofibrate | 6.9 | |||||||
Clofibric acid | 17.7-110c | NB | 17 | NB | ||||
Cortexolone | 1600-1900 | |||||||
DAUDA | 0.4-1.4 | 0.3-0.7c | ||||||
Dexamethasone | 22.1a | 41.3b | 1100-1200 | |||||
Diazepam | 0.5a | 115b | 1980-2200 NBc | NB | NB | 325 | ||
Diclofenac | 3.2a | 35b | 86.3-520c | |||||
Dilitiazem | NBc | |||||||
Fenbofibric acid | 1-1.6, 0.3a | 27.5b | 1-6.1c | 33 | 24 | 3.3 | ||
Fenofibrate | 2.9 0.02a |
0.4b | 0.8 NBc |
|||||
Fenoprofen | 14-64c | |||||||
Flufenamic acid | 3.7-15.5 | |||||||
(R/S) Flurbiprofen | 1.2a | 222b | 20-70 | |||||
Gemfibrozil | 1.9a | 179b | 110.5-121.3c | NB | 3.8 | 6.1 | ||
GW7647 | 0.3-0.6 | 1.3c | 25 | 7.6 | 0.7-8.9 | |||
(R/S) Ibuprofen | 47.6a | 448b | 32.2-263c | 325 | 2.6 | 138 | ||
3-indolacetic acid | 93-200 | |||||||
Indole-3-butyric acid | 72-170 | |||||||
Indoprofen | 1.27a | 161b | 129-520.1 | |||||
Jasmonic acid | 140-350 | |||||||
Ketoprofen | 24-82.4c | |||||||
Ketorolac | 11.6a | 119b | 9.4-2300c | |||||
Lorazepam | 12.9a | 140b | 2100-2500 | |||||
Meclofenamic acid | 0.4a | 0.3b | 8.9-21c | |||||
Mefenamic acid | 63-110 | 5.8 | 1.1 | 4.3 | ||||
Mepronil | NB | |||||||
Midazolam | 7.9 | 12 | ||||||
Nabumetone | NBc | |||||||
Nadolol | 2310 | |||||||
Nalidixic acid | NB | |||||||
2-naphthoxyacetic acid | 7.2-14 | |||||||
(S)-(-)-Naproxen | 0.06a,c | 2.8b,c | 56-180 | |||||
Nitrazepam | 1200-2300c | 28 | 36 | 20 | ||||
Perfluorononanoic acid | 1.3-3.1c | |||||||
Perfluorooctanoic acid | 2.4-6.5c | |||||||
Phenytoin | 0.2a NB |
4.7b | ||||||
Pioglitazone | 33 | NB | 11 | |||||
Prednisolone | 2.7a | 101b | 95-113 | |||||
Progesterone | 0.03 | 20-32 | ||||||
Propanolol | NB | NB | ||||||
Pyrilamine | NB | |||||||
Rosiglitazone | 2.8 | NB | NB | 28.8 | ||||
Sulfinpyrazone | 0.1c | 8.2c | ||||||
THC | 0.1-2.9 | 2.0 | 3.1 | 1 | ||||
11-COOH-THC | 11.2 NB | |||||||
11-COOH-THC-glucuronide | NB | |||||||
11-OH-THC | 5-7.2 NB | |||||||
Tolfenamic acid | 2.8-8.2c | 1.9 | 0.1 | 2.9 | ||||
Tolmetin | 1300-2200 | |||||||
Torsemide | 0.2c | 12.3c | 0.8 | |||||
Troglitazone | 1.7 | 11 | 0.02-16 | 1 | ||||
Valproate | 240-470 | |||||||
Verapamil | NB |
aAffinity for first, high affinity binding site.
bAffinity for second, low affinity binding site respectively, determined in the same study as in a.
cIncludes studies where binding affinities were determined by SPR, ITC, or thermal shift with SYPRO Orange.
CBD, cannabidiol; DAUDA, 11-(dansylamino)undecanoic acid; THC, Δ9-tetrahydrocannabinol.
NB indicates that binding was tested but no binding was observed in at least one study.
References Thumser et al., 1996; Veerkamp et al., 1999; Velkov et al., 2005, 2007, 2009; Gillilan et al., 2007; Chuang et al., 2008; Rowland et al., 2009, 2015; Trevaskis et al., 2011; Kaczocha et al., 2012; Velkov, 2013; Patil et al., 2014; Yu et al., 2014; Elmes et al., 2015, 2019; Lee et al., 2015; Sheng et al., 2016; Huang et al., 2018.