Table 1.
Receptor/mutant | Residue number | 125I-CXCL12 tracer binding (% of ACKR3) | CXCL12 |
CXCL11 |
||||||
---|---|---|---|---|---|---|---|---|---|---|
IC50 | Log IC 50 ± S.D. | EC50 | Log EC 50 ± S.D. | IC50 | Log IC 50 ± S.D. | EC50 | Log EC 50 ± S.D. | |||
% | nm | nm | nm | nm | ||||||
ACKR3 | 100 | 5.9 | −8.2 ± 0.1 | 7.0 | −8.2 ± 0.2 | 39.1 | −7.4 ± 0.2 | 9.8 | −8.1 ± 0.2 | |
D90N | 2.50 | 92 ± 13 | 12.1 | −7.9 ± 0.2 | 247 | −6.7 ± 0.3a | 35.9 | −7.5 ± 0.2 | ND | ND |
N127D | 3.35 | 70 ± 15b | 10.9 | −8.2 ± 0.2 | 226 | −6.6 ± 0.04a | 6.6a | −8.0 ± 0.2a | 906a | −6.1 ± 0.1a |
N127K | 3.35 | 83 ± 21 | 9.9 | −8.1 ± 0.2 | ND | ND | 11.0a | −7.9 ± 0.2b | ND | ND |
N127S | 3.35 | 87 ± 21 | 1.7 | −8.8 ± 0.2a | ND | ND | 3.7a | −8.5 ± 0.3a | ND | ND |
D141N | 3.49 | 64 ± 16a | 1.0 | −9.1 ± 0.3a | ND | ND | 4.8a | −8.3 ± 0.2a | ND | ND |
R142A | 3.50 | 66 ± 12a | 45.1a | −7.4 ± 0.2a | 585a | −6.2 ± 0.1a | 44.8 | −7.4 ± 0.2 | ND | ND |
Y143A | 3.51 | 93 ± 5 | 3.0 | −8.5 ± 0.1 | 493b | −6.4 ± 0.3a | 15.4c | −7.8 ± 0.1 | 436c | −6.4 ± 0.3a |
Y315A | 7.53 | 69 ± 8b | 24.7b | −7.7 ± 0.3a | ND | ND | 19.1c | −7.7 ± 0.2 | ND | ND |
a p < 0.001.
b p < 0.01.
c p < 0.05.