TABLE 3.

Association and dissociation rate constants of selected AR ligands

	Compound	Target (h, human; r, rat)	Temp (°C)	kon (M−1·min−1)	koff (min−1)	RT (min)	Kinetic KD (nM)a	Reference
7	CCPA	hA1AR	25	9.6 × 106	1.2	0.9	131	(Guo et al., 2014b)
6	NECA	hA1AR	25	9.0 × 105	0.47	2.1	522	(Guo et al., 2014b)
35	LUF5834	hA1AR	25	2.0 × 108	0.92	1.1	4.6	(Guo et al., 2014b)
36	Capadenoson	hA1AR	25	2.4 × 107	0.036	28	1.5	(Louvel et al., 2015)
37	LUF6976	hA1AR	25	3.9 × 108	0.87	1.1	2.2	(Louvel et al., 2014)
38	LUF6941	hA1AR	25	2.6 × 106	0.0076	132	2.9	(Louvel et al., 2015)
39	ABA-X-BY630	hA1ARb	37	2.6 × 107	2.0	0.5	77	(May et al., 2010)
17	DPCPX	hA1AR	25	1.4 × 108	0.21	4.8	1.5	(Guo et al., 2013)
17	DPCPX	rA1R	25	9.6 × 107	0.045	22.2	0.50	(Guo et al., 2017)
10	CGS21680	hA2AAR	25	5.0 × 104	0.02	50.0	380	(Guo et al., 2017)
10	CGS21680	rA2AAR	23	2.1 × 107	0.033	30.3	1.6	(Guo et al., 2017)
40	LUF6057	hA1AR	25	4.8 × 108	3.0	0.3	6.3	(Guo et al., 2013)
6	NECA	hA2AAR	4	1.9 × 106	0.053	19	28	(Guo et al., 2015)
11	UK432,097	hA2AAR	5	5.0 × 105	0.004	250	8.0	(Guo et al., 2012)
41	SCH58261	hA2AAR	25	6.4 × 108	1.5	0.67	2.3	(Dionisotti et al., 1997)
42	ZM241385	hA2AAR	4	1.3 × 108	0.014	71	0.11	(Guo et al., 2014c)
43	LUF6632	hA2AAR	4	3.4 × 107	0.0031	323	0.091	(Guo et al., 2014c)
20a	MSX-2	rA2AAR (brain striatal membranes)	23	14.5 × 107	0.2839	3.52	1.95	(Müller et al., 2000)
6	NECA	hA2BAR	4	n.d.	2.201	0.45	n.d.	(Hinz et al., 2018)
23	MRS1754	hA2BAR	25	2.2 × 107	0.027	37	1.2	(Ji et al., 2001)
44	MRE2029-F20	hA2BAR	4	1.7 × 107	0.031	32	1.8	(Baraldi et al., 2004)
45	OSIP339391	hA2BAR	22	9.5 × 107	0.039	26	0.41	(Stewart et al., 2004)
24	PSB-603	hA2BAR	21	11.4 × 107	0.02279	44	0.652	(Borrmann et al., 2009)
46	PSB-298	hA2BAR	25	3.76 × 107	0.9533	1.05	25	(Bertarelli et al., 2006)
47	I-AB-MECA	hA3AR	37	6.1 × 107	0.042	24	0.69	(Gao et al., 2001)
48	IB-MECA	hA3AR	10	3.5 × 107	0.011	95	0.30	(Xia et al., 2018)
14	2-Cl-IB-MECA	hA3AR	10	2.4 × 107	0.0043	231	0.18	(Xia et al., 2018)
49	MRS5127	hA3AR	25	2.4 × 108	0.51	2.0	2.1	(Auchampach et al., 2010)
16	MRS5698	hA3AR	10	7.8 × 106	5.1 × 10−4	1961	0.068	(Xia et al., 2018)
31	MRE3008-F20	hA3AR	4	7.6 × 107	0.042	24	0.55	(Varani et al., 2000)
50	LUF7531 (cmpd 2)	hA3AR	10	1.7 × 108	0.0036	315	0.021	(Xia et al., 2017)
51	PSB-11	hA3AR	25	2.35 × 108	0.2082	4.80	0.46	(Müller et al., 2002)

n.d., no data.

^a(kinetic) K_D = k_off/k_on.

^bwhole cells.