. 2020 Sep 24;15(2):155–184. doi: 10.1007/s12079-020-00585-0

Table 1.

Binding affinity (K_i) and signaling efficiency (EC₅₀) of prostanoids for the recombinant DP1 and CRTH2 (DP2) receptors expressed in cell cultures and in human platelets

	K_i (nM)
Receptor/cell line	PGD₂	PGE₂	PGF_2α	9α,11β-PGF_2α	PGJ₂	Δ¹²-PGJ₂	15-deoxy-Δ^12,14-PGJ₂	PGI₂	Reference
hDP2/K562	61 ± 23	31,000 ± 11,000	2,000 ± 780	-	460 ± 160	7,100 ± 1,600	2,300 ± 400	-	Hirai et al. 2001
hDP2/HEK293	2.4 ± 0.7	4,730 ± 64	395 ± 77	315 ± 92	6.6 ± 0.3	6.8 ± 0.35	3.2 ± 0.3	-	Sawyer et al. 2002
mDP2/HEK293	32 ± 6	-	-	-	-	-	-	-	Hata et al. 2005
mDP2/HEK293	38 ± 6	32,000 ± 400	600 ± 50	-	45.7 ± 0.2	410 ± 20	24 ± 4	-	Hata et al. 2003
hDP2/K562	61 ± 23	3,100± 1100	2,000± 780	-	460 ± 160	7,100 ± 1,300	2,300 ± 400		Hirai et al. 2001
hDP1/K562	45 ± 17	2,300± 1100	>30,000	-	64 ± 13	5,200 ± 1,700	30,000	-	Hirai et al. 2001
hDP1/COS M-6^a	1.1	101	1,000	-	-	-	-	-	Boie et al. 1995
hDP1/HEK293	0.6 ± 0.2	107 ± 42	367 ± 85	-	6.6± 0.3	100 ± 13	280 ± 30	-	Wright et al. 1998
hDP1/HEK293	1.7 ± 0.3	307± 106	861 ± 139	-	-	-	-	-	Sawyer et al. 2002
DP/human platelets	81 ± 5	>10,000	18,000 ± 6,460	-	-	-	-	3537	Sharif et al. 2003
DP/human platelets	80.3 ± 5.5	11,000 ± 2,190	32,000 ± 3,500	-	-	-	-	-	Sharif et al. 2000a
DP/human platelets	80 ± 5	11,000 ± 2,100	18,000 ± 6,400	-	-	-	-	-	Sharif et al. 2000b
	EC₅₀ (nM)
Receptor/cell line	PGD₂	PGE₂	PGF_2α	9α,11β-PGF_2α	PGJ₂	Δ¹²-PGJ₂	15-deoxy-Δ^12,14-PGJ₂	PGI₂	Reference
hDP2/HEK293^b	1.6± 0.3	-	456 ± 169	856 ± 322	13.1 ± 5.36	10.8 ± 3.4	11.6 ± 6.3	-	Sawyer et al. 2002
mDP2/HEK293	0.7 ± 0.3	-	-	-	-	-	-	-	Hata et al. 2005
mDP2/HEK293	0.9 ± 0.2	-	-	-	-	-	0.8 ± 0.3	-	Hata et al. 2003
hDP1/HEK293	1.38 ± 0.785	206 ± 156	1,090 ± 975	-	-	-	-	-	Suganami et al. 2016
hDP1/HEK293^a	10	500	1000	-	-	-	-	-	Boie et al. 1995
hDP1/HEK293	0.5 ± 0.1	84 ± 1	264 ± 22	-	1.2 ± 0.1	91 ± 18	321 ± 15	-	Wright et al. 1998
bDP/EbTr	74	>1,000	>10,000	-	-	-	-	>10,000	Sharif et al. 2003
hDP/human platelets	98 ± 10	>10,000	>10,000	-	-	-	-	-	Sharif et al. 2000b

Abbreviations: h, human; m, mouse; b, bovine; HEK293, human embryonic kidney cells; K562, human erythroleukemia cells; COS M-6, Green monkey kidney cells; EbTr, bovine embryonic tracheal cells. The K_i values were determined from [³H]PGD₂ displacement assays. The EC₅₀ determined from intracellular changes in cAMP concentrations. a) Values determined from estimated IC₅₀ taken from binding curves, utilizing the Cheng-Prusoff equation (Suganami et al. 2016); b) Ca²⁺ concentrations also measured.