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Assay Detail

CHEMBL2351084

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]-IL8 from human CXCR2 transfected in HEK293 cells after 4 hrs by microbeta counting analysis
ChEMBL ↗
51
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 2 (CHEMBL2434) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1).
Karlström S, Nordvall G, Sohn D, Hettman A, Turek D, Åhlin K, Kers A, Claesson M, Slivo C, Lo-Alfredsson Y, Petersson C, Bessidskaia G, Svensson PH, Rein T, Jerning E, Malmberg Å, Ahlgen C, Ray C, Vares L, Ivanov V, Johansson R.
J Med Chem (2013) 56 : 3177 -3190
PubMed 23516963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 49 6.17 8.39
IC50 2 8.12 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349306 — — 1 8.39
CHEMBL402986 — — 1 8.35
CHEMBL271013 — — 1 7.89
CHEMBL2349334 — — 1 7.68
CHEMBL2349307 — — 1 7.19
CHEMBL2349321 — — 1 7.10
CHEMBL2349333 — — 1 7.10
CHEMBL2349184 — — 1 7.00
CHEMBL2349338 — — 1 6.82
CHEMBL274737 — — 1 6.80
CHEMBL2349328 — — 1 6.72
CHEMBL2349312 — — 1 6.68
CHEMBL2349324 — — 1 6.66
CHEMBL2349181 — — 1 6.66
CHEMBL2349331 — — 1 6.59
CHEMBL2349182 — — 1 6.46
CHEMBL2349320 — — 1 6.43
CHEMBL2349185 — — 1 6.34
CHEMBL2349180 — — 1 6.31
CHEMBL2349339 — — 1 6.29
CHEMBL2349183 — — 1 6.28
CHEMBL2349335 — — 1 6.28
CHEMBL2349332 — — 1 6.25
CHEMBL2349186 — — 1 6.24
CHEMBL2349327 — — 1 6.23
CHEMBL2349318 — — 1 6.04
CHEMBL2349179 — — 1 5.95
CHEMBL2349313 — — 1 5.87
CHEMBL2349316 — — 1 5.85
CHEMBL2349325 — — 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349306 — Ki = 4.1 nM 8.39
CHEMBL402986 — IC50 = 4.5 nM 8.35
CHEMBL271013 — IC50 = 13.0 nM 7.89
CHEMBL2349334 — Ki = 21.0 nM 7.68
CHEMBL2349307 — Ki = 64.0 nM 7.19
CHEMBL2349321 — Ki = 79.0 nM 7.10
CHEMBL2349333 — Ki = 79.0 nM 7.10
CHEMBL2349184 — Ki = 100.0 nM 7.00
CHEMBL2349338 — Ki = 150.0 nM 6.82
CHEMBL274737 — Ki = 160.0 nM 6.80
CHEMBL2349328 — Ki = 190.0 nM 6.72
CHEMBL2349312 — Ki = 210.0 nM 6.68
CHEMBL2349324 — Ki = 220.0 nM 6.66
CHEMBL2349181 — Ki = 220.0 nM 6.66
CHEMBL2349331 — Ki = 258.0 nM 6.59
CHEMBL2349182 — Ki = 349.0 nM 6.46
CHEMBL2349320 — Ki = 370.0 nM 6.43
CHEMBL2349185 — Ki = 460.0 nM 6.34
CHEMBL2349180 — Ki = 489.0 nM 6.31
CHEMBL2349339 — Ki = 510.0 nM 6.29
CHEMBL2349183 — Ki = 523.0 nM 6.28
CHEMBL2349335 — Ki = 530.0 nM 6.28
CHEMBL2349332 — Ki = 567.0 nM 6.25
CHEMBL2349186 — Ki = 580.0 nM 6.24
CHEMBL2349327 — Ki = 590.0 nM 6.23
CHEMBL2349318 — Ki = 920.0 nM 6.04
CHEMBL2349179 — Ki = 1129.0 nM 5.95
CHEMBL2349313 — Ki = 1360.0 nM 5.87
CHEMBL2349316 — Ki = 1400.0 nM 5.85
CHEMBL2349325 — Ki = 1500.0 nM 5.82
CHEMBL2349330 — Ki = 1600.0 nM 5.80
CHEMBL2349322 — Ki = 1750.0 nM 5.76
CHEMBL2349323 — Ki = 1790.0 nM 5.75
CHEMBL2349303 — Ki = 1940.0 nM 5.71
CHEMBL2349329 — Ki = 1980.0 nM 5.70
CHEMBL2349311 — Ki = 2100.0 nM 5.68
CHEMBL2349304 — Ki = 2400.0 nM 5.62
CHEMBL2349314 — Ki = 2600.0 nM 5.58
CHEMBL2349310 AZD-8797 Ki = 2800.0 nM 5.55
CHEMBL2349326 — Ki = 4100.0 nM 5.39
CHEMBL2349302 — Ki = 4200.0 nM 5.38
CHEMBL2349308 — Ki = 5400.0 nM 5.27
CHEMBL2349305 — Ki = 5900.0 nM 5.23
CHEMBL2349315 — Ki = 6000.0 nM 5.22
CHEMBL2349309 — Ki = 9000.0 nM 5.05
CHEMBL2349317 — Ki = 13000.0 nM 4.89
CHEMBL2349337 — Ki - — -
CHEMBL2349336 — Ki - — -
CHEMBL2349319 — Ki > 100000.0 nM -
CHEMBL2349187 — Ki - — -