Template:Affinities of 5α-dihydroethisterone for steroid hormone proteins
AR | ERα | ERβ | PR | GR | SHBG | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|
IC50 | RBA | IC50 | RBA | IC50 | RBA | IC50 | RBA | IC50 | RBA | Kd | RBA |
0.5–16 nM | 38–100% | 229 nM | 3.5% | >10,000 nM | IA | 130 nM | 12% | 7 nM | 120% | 0.18 nM | 100% |
Notes: IC50 values are for binding inhibition (affinity). Reference ligands for RBA (100%) were DHT for the AR, estradiol for the ERα and ERβ, progesterone for the PR, dexamethasone for the GR, and DHT for SHBG. Sources: [1][2][3][4][5] |

References
- ↑ Lemus AE, Enríquez J, García GA, Grillasca I, Pérez-Palacios G (January 1997). "5alpha-reduction of norethisterone enhances its binding affinity for androgen receptors but diminishes its androgenic potency". J. Steroid Biochem. Mol. Biol. 60 (1–2): 121–9. doi:10.1016/S0960-0760(96)00172-0. PMID 9182866.
- ↑ Ahlem C, Kennedy M, Page T, Bell D, Delorme E, Villegas S, Reading C, White S, Stickney D, Frincke J (February 2012). "17α-alkynyl 3α, 17β-androstanediol non-clinical and clinical pharmacology, pharmacokinetics and metabolism". Invest New Drugs. 30 (1): 59–78. doi:10.1007/s10637-010-9517-0. PMID 20814732.
- ↑ Cunningham GR, Lobl TJ, Cockrell C, Shao TC, Tindall DJ (May 1983). "Characterization of steroid binding specificity of the androgen receptor in human foreskin fibroblasts". Steroids. 41 (5): 617–26. doi:10.1016/0039-128X(83)90027-2. PMID 6658893.
- ↑ Cunningham GR, Tindall DJ, Lobl TJ, Campbell JA, Means AR (September 1981). "Steroid structural requirements for high affinity binding to human sex steroid binding protein (SBP)". Steroids. 38 (3): 243–62. doi:10.1016/0039-128X(81)90061-1. PMID 7197818.
- ↑ Cherkasov A, Ban F, Santos-Filho O, Thorsteinson N, Fallahi M, Hammond GL (April 2008). "An updated steroid benchmark set and its application in the discovery of novel nanomolar ligands of sex hormone-binding globulin". J. Med. Chem. 51 (7): 2047–56. doi:10.1021/jm7011485. PMID 18330978.
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