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Assay Detail

CHEMBL2050319

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Binding
Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells
ChEMBL ↗
70
Total Activities
70
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

Histamine H4 receptor (CHEMBL3759) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.
Engelhardt H, de Esch IJ, Kuhn D, Smits RA, Zuiderveld OP, Dobler J, Mayer M, Lips S, Arnhof H, Scharn D, Haaksma EE, Leurs R.
Eur J Med Chem (2012) 54 : 660 -668
PubMed 22749391 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 70 6.85 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2047450 — — 1 8.30
CHEMBL129198 JNJ-7777120 — 1 8.20
CHEMBL2047449 — — 1 8.20
CHEMBL2047448 — — 1 8.20
CHEMBL129436 — — 1 8.20
CHEMBL2047447 — — 1 8.20
CHEMBL2047466 — — 1 8.00
CHEMBL503605 — — 1 7.90
CHEMBL2047451 — — 1 7.90
CHEMBL129488 — — 1 7.90
CHEMBL129540 — — 1 7.80
CHEMBL436381 — — 1 7.80
CHEMBL2047470 — — 1 7.80
CHEMBL2047473 — — 1 7.70
CHEMBL2047276 — — 1 7.70
CHEMBL338051 — — 1 7.70
CHEMBL129199 — — 1 7.60
CHEMBL2047273 — — 1 7.60
CHEMBL128958 — — 1 7.60
CHEMBL340740 — — 1 7.50
CHEMBL2047263 — — 1 7.50
CHEMBL2047469 — — 1 7.50
CHEMBL2047454 — — 1 7.50
CHEMBL2047264 — — 1 7.50
CHEMBL2047475 — — 1 7.40
CHEMBL2047443 — — 1 7.40
CHEMBL2047462 — — 1 7.40
CHEMBL2047455 — — 1 7.40
CHEMBL128088 — — 1 7.30
CHEMBL2047468 — — 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2047450 — Ki = 5.012 nM 8.30
CHEMBL129198 JNJ-7777120 Ki = 6.31 nM 8.20
CHEMBL2047447 — Ki = 6.31 nM 8.20
CHEMBL129436 — Ki = 6.31 nM 8.20
CHEMBL2047449 — Ki = 6.31 nM 8.20
CHEMBL2047448 — Ki = 6.31 nM 8.20
CHEMBL2047466 — Ki = 10.0 nM 8.00
CHEMBL503605 — Ki = 12.59 nM 7.90
CHEMBL2047451 — Ki = 12.59 nM 7.90
CHEMBL129488 — Ki = 12.59 nM 7.90
CHEMBL129540 — Ki = 15.85 nM 7.80
CHEMBL436381 — Ki = 15.85 nM 7.80
CHEMBL2047470 — Ki = 15.85 nM 7.80
CHEMBL2047473 — Ki = 19.95 nM 7.70
CHEMBL2047276 — Ki = 19.95 nM 7.70
CHEMBL338051 — Ki = 19.95 nM 7.70
CHEMBL129199 — Ki = 25.12 nM 7.60
CHEMBL2047273 — Ki = 25.12 nM 7.60
CHEMBL128958 — Ki = 25.12 nM 7.60
CHEMBL340740 — Ki = 31.62 nM 7.50
CHEMBL2047263 — Ki = 31.62 nM 7.50
CHEMBL2047469 — Ki = 31.62 nM 7.50
CHEMBL2047454 — Ki = 31.62 nM 7.50
CHEMBL2047264 — Ki = 31.62 nM 7.50
CHEMBL2047455 — Ki = 39.81 nM 7.40
CHEMBL2047443 — Ki = 39.81 nM 7.40
CHEMBL2047475 — Ki = 39.81 nM 7.40
CHEMBL2047462 — Ki = 39.81 nM 7.40
CHEMBL128088 — Ki = 50.12 nM 7.30
CHEMBL2047468 — Ki = 63.1 nM 7.20
CHEMBL2047467 — Ki = 63.1 nM 7.20
CHEMBL2047476 — Ki = 79.43 nM 7.10
CHEMBL2047446 — Ki = 79.43 nM 7.10
CHEMBL2047275 — Ki = 79.43 nM 7.10
CHEMBL2047270 — Ki = 79.43 nM 7.10
CHEMBL2047463 — Ki = 100.0 nM 7.00
CHEMBL2047471 — Ki = 100.0 nM 7.00
CHEMBL2047272 — Ki = 158.49 nM 6.80
CHEMBL2047266 — Ki = 158.49 nM 6.80
CHEMBL2047453 — Ki = 199.53 nM 6.70
CHEMBL2047259 — Ki = 251.19 nM 6.60
CHEMBL2047452 — Ki = 251.19 nM 6.60
CHEMBL2047458 — Ki = 251.19 nM 6.60
CHEMBL2047472 — Ki = 251.19 nM 6.60
CHEMBL2047268 — Ki = 316.23 nM 6.50
CHEMBL2047445 — Ki = 398.11 nM 6.40
CHEMBL2047465 — Ki = 398.11 nM 6.40
CHEMBL2047460 — Ki = 398.11 nM 6.40
CHEMBL2047456 — Ki = 398.11 nM 6.40
CHEMBL2047474 — Ki = 398.11 nM 6.40