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Assay Detail

CHEMBL4416273

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

Binding
Displacement of PPHT-red from SNAP-tagged human D2LR expressed in CHOK1 cell membranes by TR-FRET assay
ChEMBL ↗
102
Total Activities
51
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

D(2) dopamine receptor (CHEMBL217) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.
Fyfe TJ, Kellam B, Sykes DA, Capuano B, Scammells PJ, Lane JR, Charlton SJ, Mistry SN.
J Med Chem (2019) 62 : 9488 -9520
PubMed 31580666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 51 8.21 10.26
Ki 51 8.23 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451384 — — 2 10.28
CHEMBL4570273 — — 2 9.92
CHEMBL4544491 — — 2 9.84
CHEMBL4528835 — — 2 9.84
CHEMBL4436610 — — 2 9.49
CHEMBL4436241 — — 2 9.35
CHEMBL54 HALOPERIDOL 4.0 2 9.33
CHEMBL2104700 MOPERONE 2.0 2 9.14
CHEMBL1940404 — — 2 9.10
CHEMBL4455788 — — 2 9.00
CHEMBL4529368 — — 2 8.99
CHEMBL4453290 — — 2 8.83
CHEMBL4472382 — — 2 8.82
CHEMBL147830 — — 2 8.76
CHEMBL199226 — — 2 8.75
CHEMBL422334 — — 2 8.73
CHEMBL1940403 — — 2 8.71
CHEMBL4475608 — — 2 8.71
CHEMBL4540679 — — 2 8.67
CHEMBL4444768 — — 2 8.62
CHEMBL4472206 — — 2 8.61
CHEMBL4461948 — — 2 8.52
CHEMBL4472585 — — 2 8.47
CHEMBL363548 CHLOROHALOPERIDOL — 2 8.30
CHEMBL4568709 — — 2 8.28
CHEMBL1940402 — — 2 8.27
CHEMBL4463187 — — 2 8.13
CHEMBL54206 — — 2 8.12
CHEMBL56843 — — 2 8.11
CHEMBL4514517 — — 2 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451384 — Ki = 0.05248 nM 10.28
CHEMBL4451384 — Kd = 0.05495 nM 10.26
CHEMBL4570273 — Ki = 0.1202 nM 9.92
CHEMBL4570273 — Kd = 0.1445 nM 9.84
CHEMBL4544491 — Kd = 0.1445 nM 9.84
CHEMBL4528835 — Kd = 0.1445 nM 9.84
CHEMBL4544491 — Ki = 0.1549 nM 9.81
CHEMBL4528835 — Ki = 0.1585 nM 9.80
CHEMBL4436610 — Ki = 0.3236 nM 9.49
CHEMBL4436241 — Ki = 0.4467 nM 9.35
CHEMBL4436610 — Kd = 0.4571 nM 9.34
CHEMBL54 HALOPERIDOL Ki = 0.4677 nM 9.33
CHEMBL54 HALOPERIDOL Kd = 0.4898 nM 9.31
CHEMBL4436241 — Kd = 0.537 nM 9.27
CHEMBL2104700 MOPERONE Ki = 0.7244 nM 9.14
CHEMBL1940404 — Kd = 0.7943 nM 9.10
CHEMBL2104700 MOPERONE Kd = 0.955 nM 9.02
CHEMBL4455788 — Kd = 1.0 nM 9.00
CHEMBL4455788 — Ki = 1.0 nM 9.00
CHEMBL4529368 — Ki = 1.023 nM 8.99
CHEMBL4529368 — Kd = 1.047 nM 8.98
CHEMBL1940404 — Ki = 1.072 nM 8.97
CHEMBL4453290 — Ki = 1.479 nM 8.83
CHEMBL4472382 — Ki = 1.514 nM 8.82
CHEMBL4472382 — Kd = 1.514 nM 8.82
CHEMBL147830 — Ki = 1.738 nM 8.76
CHEMBL199226 — Ki = 1.778 nM 8.75
CHEMBL199226 — Kd = 1.778 nM 8.75
CHEMBL422334 — Kd = 1.862 nM 8.73
CHEMBL422334 — Ki = 1.905 nM 8.72
CHEMBL147830 — Kd = 1.905 nM 8.72
CHEMBL4475608 — Kd = 1.95 nM 8.71
CHEMBL1940403 — Kd = 1.95 nM 8.71
CHEMBL1940403 — Ki = 2.089 nM 8.68
CHEMBL4453290 — Kd = 2.089 nM 8.68
CHEMBL4540679 — Ki = 2.138 nM 8.67
CHEMBL4444768 — Kd = 2.399 nM 8.62
CHEMBL4472206 — Ki = 2.455 nM 8.61
CHEMBL4444768 — Ki = 2.63 nM 8.58
CHEMBL4472206 — Kd = 2.692 nM 8.57
CHEMBL4461948 — Kd = 3.02 nM 8.52
CHEMBL4540679 — Kd = 3.236 nM 8.49
CHEMBL4461948 — Ki = 3.311 nM 8.48
CHEMBL4472585 — Kd = 3.388 nM 8.47
CHEMBL4475608 — Ki = 3.548 nM 8.45
CHEMBL4472585 — Ki = 3.548 nM 8.45
CHEMBL363548 CHLOROHALOPERIDOL Ki = 5.012 nM 8.30
CHEMBL363548 CHLOROHALOPERIDOL Kd = 5.012 nM 8.30
CHEMBL4568709 — Ki = 5.248 nM 8.28
CHEMBL1940402 — Ki = 5.37 nM 8.27