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Assay Detail

CHEMBL2351085

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

Binding
Displacement of [125I]-CX3CL1 from human CX3CR1 transfected in HEK293 cells after 24 hrs by scintillation counting analysis
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
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

CX3C chemokine receptor 1 (CHEMBL4843) ↗
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 51 7.14 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349310 AZD-8797 2.0 1 8.41
CHEMBL2349322 — — 1 8.40
CHEMBL2349316 — — 1 8.33
CHEMBL2349180 — — 1 8.24
CHEMBL2349179 — — 1 8.21
CHEMBL2349312 — — 1 8.11
CHEMBL2349313 — — 1 8.10
CHEMBL2349332 — — 1 8.09
CHEMBL2349303 — — 1 8.08
CHEMBL2349306 — — 1 8.00
CHEMBL2349314 — — 1 7.89
CHEMBL2349318 — — 1 7.85
CHEMBL2349311 — — 1 7.75
CHEMBL2349182 — — 1 7.75
CHEMBL2349181 — — 1 7.68
CHEMBL2349324 — — 1 7.64
CHEMBL2349319 — — 1 7.55
CHEMBL2349321 — — 1 7.52
CHEMBL2349328 — — 1 7.50
CHEMBL2349317 — — 1 7.38
CHEMBL2349302 — — 1 7.37
CHEMBL2349186 — — 1 7.36
CHEMBL2349330 — — 1 7.33
CHEMBL2349335 — — 1 7.32
CHEMBL2349323 — — 1 7.29
CHEMBL2349325 — — 1 7.16
CHEMBL2349333 — — 1 7.15
CHEMBL2349329 — — 1 7.04
CHEMBL2349301 — — 1 7.04
CHEMBL2349327 — — 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349310 AZD-8797 Ki = 3.9 nM 8.41
CHEMBL2349322 — Ki = 4.0 nM 8.40
CHEMBL2349316 — Ki = 4.7 nM 8.33
CHEMBL2349180 — Ki = 5.8 nM 8.24
CHEMBL2349179 — Ki = 6.2 nM 8.21
CHEMBL2349312 — Ki = 7.8 nM 8.11
CHEMBL2349313 — Ki = 8.0 nM 8.10
CHEMBL2349332 — Ki = 8.1 nM 8.09
CHEMBL2349303 — Ki = 8.3 nM 8.08
CHEMBL2349306 — Ki = 10.0 nM 8.00
CHEMBL2349314 — Ki = 13.0 nM 7.89
CHEMBL2349318 — Ki = 14.0 nM 7.85
CHEMBL2349311 — Ki = 18.0 nM 7.75
CHEMBL2349182 — Ki = 18.0 nM 7.75
CHEMBL2349181 — Ki = 21.0 nM 7.68
CHEMBL2349324 — Ki = 23.0 nM 7.64
CHEMBL2349319 — Ki = 28.0 nM 7.55
CHEMBL2349321 — Ki = 30.0 nM 7.52
CHEMBL2349328 — Ki = 32.0 nM 7.50
CHEMBL2349317 — Ki = 42.0 nM 7.38
CHEMBL2349302 — Ki = 43.0 nM 7.37
CHEMBL2349186 — Ki = 44.0 nM 7.36
CHEMBL2349330 — Ki = 47.0 nM 7.33
CHEMBL2349335 — Ki = 48.0 nM 7.32
CHEMBL2349323 — Ki = 51.0 nM 7.29
CHEMBL2349325 — Ki = 70.0 nM 7.16
CHEMBL2349333 — Ki = 71.0 nM 7.15
CHEMBL2349329 — Ki = 91.0 nM 7.04
CHEMBL2349301 — Ki = 91.0 nM 7.04
CHEMBL2349327 — Ki = 99.0 nM 7.00
CHEMBL2349339 — Ki = 100.0 nM 7.00
CHEMBL2349315 — Ki = 102.0 nM 6.99
CHEMBL2349183 — Ki = 110.0 nM 6.96
CHEMBL2349184 — Ki = 110.0 nM 6.96
CHEMBL2349326 — Ki = 120.0 nM 6.92
CHEMBL2349320 — Ki = 190.0 nM 6.72
CHEMBL2349337 — Ki = 220.0 nM 6.66
CHEMBL2349304 — Ki = 220.0 nM 6.66
CHEMBL2349185 — Ki = 280.0 nM 6.55
CHEMBL2349305 — Ki = 320.0 nM 6.50
CHEMBL2349307 — Ki = 360.0 nM 6.44
CHEMBL2349334 — Ki = 560.0 nM 6.25
CHEMBL2349336 — Ki = 600.0 nM 6.22
CHEMBL2349338 — Ki = 640.0 nM 6.19
CHEMBL2349308 — Ki = 670.0 nM 6.17
CHEMBL274737 — Ki = 770.0 nM 6.11
CHEMBL2349309 — Ki = 900.0 nM 6.05
CHEMBL271013 — Ki = 1100.0 nM 5.96
CHEMBL2349331 — Ki = 1200.0 nM 5.92
CHEMBL2349187 — Ki = 1200.0 nM 5.92