Transporter Herbal compound Substrate/ Inhibitor IC50
(μM)
Ki
(μM)
Km
(μM)
Reference
OATP2B1 Ursolic acid Inhibitor 11.0 ± 5.0 ND ND [19]
  Baicalin Inhibitor 5.6 ± 3.2 ND ND [33]
  Baicalein Inhibitor ND ND ND [33]
  Wogonin Inhibitor ND ND ND [33]
  Icariin Inhibitor 6.4 ± 1.9 ND ND [78]
  Silybin A Inhibitor 4.5 ND ND [80]
  Silybin B Inhibitor 0.8 ND ND [80]
  Silychristin Inhibitor 3.6 ND ND [80]
OATP1B3 Gallic acid Inhibitor 1.6 ± 0.6 ND ND [19]
  Baicalin Inhibitor 13.7 ± 3.6 ND ND [33]
  Baicalein Inhibitor 7.7 ± 2.4 ND ND [33]
  Wogonin Inhibitor 7.7 ± 3.1 ND ND [33]
  Icariin Inhibitor 3.0 ± 1.3 ND ND [78]
  Silybin A Inhibitor 2.7 ND ND [80]
  Silybin B Inhibitor 5.0 ND ND [80]
  Silychristin Inhibitor 36.4 ND ND [80]
  Epicatechin-gallate Substrate ND ND 34.1 [81]
  Epigallocate-chin gallate Substrate ND ND 13.2 [81]
  Dioscin Substrate ND ND 2.08 ± 0.27 [84]
OATP1B1 Baicalin Inhibitor 121.0 ± 9.3 ND ND [33]
  Baicalein Inhibitor 172.6 ± 6.3 ND ND [33]
  Wogonin Inhibitor >200 ND ND [33]
  Icariin Inhibitor 21.9 ± 2.0 ND ND [23]
  Silybin A Inhibitor 9.7 ND ND [80]
  Silybin B Inhibitor 8.5 ND ND [80]
  Silychristin Inhibitor 9.0 ND ND [80]
  Periplocin Inhibitor ND ND ND [85]
  Epigallocatechingallate Inhibitor 7.8 ND ND [81]
OATP1A2 Epicatechingallate Substrate 10.2 ND 10.4 [81]
  Epigallocatechingallate Substrate 54.8 ND 18.8 [81]
  Quercetin Substrate ND ND 2.3 ± 1.5 [83]
OATP4C1 3-monoglucuronyl-glycyrrhetinic acid Substrate ND ND 33.1 [43]
ND: not determined
Table 3: The interactions of herbal compounds with human OATPs.